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:
March 13, 2013
Date of Patent:
July 15, 2014
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
Abstract: The present invention relates to processes and intermediates for the preparation of compounds useful as CRTH2 antagonists. Compounds prepared by the processes of the invention are of Formula (AI), (All) and Compound (I).
Type:
Application
Filed:
June 17, 2011
Publication date:
July 3, 2014
Applicant:
Ironwood Pharmaceuticals, Inc.
Inventors:
James Jia, Regina Graul, Wayne C Schairer, Vishnu Karnati, Ray Forslund
Abstract: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
Type:
Application
Filed:
November 14, 2013
Publication date:
June 26, 2014
Applicant:
IMMUNOGEN, INC.
Inventors:
Ravi V.J. Chari, Robert Yongxin Zhao, Yelena Kovtun, Rajeeva Singh, Wayne C. Widdison
Abstract: A method of servicing a wellbore in a subterranean formation comprising placing a composition comprising a carrier fluid and a degradable polymer into the subterranean formation wherein the degradable polymer comprises polyimide, allowing the degradable polymer to form a diverter plug at a first location in the wellbore or subterranean formation, diverting the flow of a wellbore servicing fluid to a second location in the wellbore or subterranean formation that is different than the first location; and removing all or a portion of the diverter plug by contacting the diverter plug with a degradation accelerator wherein the degradation accelerator comprises an amino alcohol, an amino alcohol precursor, an organic amine, an organic amine precursor or combinations thereof. A wellbore servicing fluid comprising polysuccinimide wherein the wellbores servicing fluid has a pH of less than about 7.
Abstract: The current application relates to a metal catalyst of formula (I): M[ADC][X]n, wherein M is a metal, ADC is a chiral acyclic diaminocarbene ligand, and X is a neutral or anionic ligand. The ADC ligand is prepared from the corresponding chiral formamidium salt precursor. The metal catalyst is used for asymmetric organic synthesis reactions such as hydrosilations, hydrogenations, conjugate additions, and cross-couplings.
Type:
Grant
Filed:
July 7, 2009
Date of Patent:
June 24, 2014
Inventors:
Avinash N. Thadani, Rukundo Ntaganda, Mira M. Beshai
Abstract: The present disclosure relates to a series of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I). wherein R, R1, R2, R3, R4, X, m, n and p 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 disclosure relates to methods of preparation of substituted N-heterocycloalkyl bipyrrolidinylphenyl amide derivatives of formula (I) and intermediates therefor.
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.
Type:
Grant
Filed:
March 13, 2013
Date of Patent:
June 10, 2014
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. Macielag
Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
Type:
Application
Filed:
November 22, 2013
Publication date:
June 5, 2014
Applicant:
ABBVIE INC.
Inventors:
David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
Abstract: A compound having a structure expressed by the following Structural Formula (1), tautomers thereof, or salts of the compound or the tautomers.
Abstract: The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.
Type:
Grant
Filed:
April 5, 2010
Date of Patent:
May 27, 2014
Assignee:
PTC Therapeutics, Inc.
Inventors:
Malcolm MacCoss, F. George Njoroge, Amin Nomeir, Guangming Chen, Song Xiao Huang, Ramesh Kakarla, Gary Mitchell Karp, William Joseph Lennox, Chunshi Li, Ronggang Liu, Yalei Liu, Christie Morrill, Steven D. Paget, Sean W Smith, James Takasugi, Anthony A. Turpoff, Hongyu Ren, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
Type:
Application
Filed:
April 13, 2012
Publication date:
May 22, 2014
Applicant:
PHENEX PHARMACEUTICALS AG
Inventors:
Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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:
December 20, 2012
Date of Patent:
May 20, 2014
Assignee:
Incyte Corporation
Inventors:
Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
Abstract: Compound with formula (I), wherein R? and R? represent a hydrogen atom, a monovalent radical with formula (IIa), or a monovalent radical with formula (IIb), it being understood that at least one of the R? or R? radicals does not represent a hydrogen atom and that when the R? and R? radicals do not represent a hydrogen atom, R? and R? are identical; method for preparing and using in cosmetics and as a drug.
Type:
Application
Filed:
May 24, 2012
Publication date:
May 15, 2014
Applicant:
SOCIETE D'EXPLOITATION DE PROUITS POUR LES INDUSTRIES CHMIQUES SEPPIC
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 the compounds.
Type:
Grant
Filed:
September 10, 2010
Date of Patent:
April 22, 2014
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
Abstract: Methods for deposition of elemental metal films on surfaces using metal coordination complexes comprising nitrogen-containing ligands are provided. Also provided are nitrogen-containing ligands useful in the methods of the invention and metal coordination complexes comprising these ligands.
Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Z 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 modulators 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:
November 19, 2008
Date of Patent:
April 15, 2014
Assignee:
Incyte Corporation
Inventors:
Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
Type:
Grant
Filed:
February 12, 2013
Date of Patent:
April 1, 2014
Assignee:
Janssen Pharmaceutica NV
Inventors:
Frank Chavez, James P. Edwards, Brad M. Savall, Jianmei Wei, Ronald L. Wolin
Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Application
Filed:
August 29, 2013
Publication date:
March 6, 2014
Inventors:
Stefan SCHUNK, Melanie REICH, Henning STEINHAGEN, Nils DAMANN, Michael HAURAND, Achim KLESS, Philip SKONE, Richard HAMLYN, Robert KIRBY, Marc ROGERS, Kathy SUTTON
Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
Type:
Grant
Filed:
February 3, 2011
Date of Patent:
February 25, 2014
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Grant
Filed:
August 31, 2012
Date of Patent:
February 25, 2014
Assignee:
Hoffmann-LaRoche Inc.
Inventors:
Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
December 22, 2011
Date of Patent:
February 11, 2014
Assignees:
Cephalon, Inc., Teva Sante
Inventors:
Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
February 4, 2014
Assignees:
Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
Inventors:
Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
Type:
Grant
Filed:
April 3, 2012
Date of Patent:
January 28, 2014
Assignee:
AbbVie Inc.
Inventors:
David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
Abstract: Provided are tetrakis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders.
Type:
Grant
Filed:
October 29, 2008
Date of Patent:
January 14, 2014
Assignee:
University of Kentucky Research Foundation
Inventors:
Peter A. Crooks, Linda P. Dwoskin, Zhenfa Zhang, Marharyta Pivavarchyk
Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 14, 2012
Date of Patent:
January 7, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Fleck, Bernd Nosse, Gerald Juergen Roth
Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides 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 N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
Type:
Grant
Filed:
March 15, 2010
Date of Patent:
December 31, 2013
Assignee:
Sanofi
Inventors:
Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
Type:
Application
Filed:
August 2, 2013
Publication date:
December 5, 2013
Applicant:
Gilead Sciences, Inc.
Inventors:
Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman Belmont, Philip Anthony Morganelli, William J. Watkins
Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example inflammatory conditions, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
Type:
Application
Filed:
January 10, 2012
Publication date:
November 14, 2013
Inventors:
Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédicte Pourbaix-L'ebraly
Abstract: Disclosed are functionalized expanded porphyrins that can be used as spectrometric sensors for high-valent actinide cations. The disclosed functionalized expanded porphyrins have the advantage over unfunctionalized systems in that they can be immobilized via covalent attachment to a solid support comprising an inorganic or organic polymer or other common substrates. Substrates comprising the disclosed functionalized expanded porphyrins are also disclosed. Further, disclosed are methods of making the disclosed compounds (immobilized and free), methods of using them as sensors to detect high valent actinides, devices that comprise the disclosed compounds, and kits.
Type:
Grant
Filed:
June 23, 2008
Date of Patent:
November 12, 2013
Assignee:
Board of Regents, The University of Texas System
Inventors:
Jonathan L. Sessler, Patricia J. Pantos
Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
Type:
Grant
Filed:
April 19, 2011
Date of Patent:
November 5, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Harald Engelhardt, Christiane Kofink, Darryl McConnell
Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
Abstract: The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R5 is hydrogen or a C1-C7 linear or branched acyclic hydrocarbon group, or R5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R1, and R2 are defined herein.
Type:
Grant
Filed:
October 20, 2011
Date of Patent:
November 5, 2013
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Yue-Mei Zhang, Peter J. Connolly, Shu-Chen Lin, Mark J. MacIelag
Abstract: Provided herein are compounds and methods of using same for the perturbation and/or inhibition of protein-protein interactions. Also provided herein is a data mining method useful for the identification of protein-protein interactions that may be inhibited by these compounds.
Abstract: A process for inhibiting polymerization of an aromatic vinyl compound during the stage of producing, purifying, storing or transporting the aromatic vinyl compound which not only inhibits an initial polymerization but also inhibits polymerization efficiently over a long period of time and which is excellent in handleability. The process involves the step of adding a nitrogenous aromatic compound in combination with a sulfonic acid compound to the aromatic vinyl compound during the production, purification, storage of transportation thereof.
Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
Type:
Grant
Filed:
July 5, 2011
Date of Patent:
October 1, 2013
Assignee:
AstraZeneca AB
Inventors:
Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
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
Abstract: The present invention relates to compounds from Antrodia cinnamomea. The present invention also relates to a composition and a method for treating or prophylaxis of hepatitis C virus (HCV) or human immunodeficiency virus (HIV) infection.
Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
Type:
Grant
Filed:
October 23, 2009
Date of Patent:
August 27, 2013
Assignee:
Virobay, Inc.
Inventors:
Michael Graupe, John O. Link, Chandrasekar Venkataramani
Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
Type:
Grant
Filed:
April 26, 2010
Date of Patent:
August 20, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt 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).
Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Application
Filed:
December 14, 2012
Publication date:
July 4, 2013
Inventors:
Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
Abstract: The present invention relates to novel dihydropyrido[4,3 -b]pyrazin-3(4H)-ones of the general formula: useful as modulators of toll-like receptors, and to pharmaceutical compositions containing them.
Abstract: Fullerene surfactant compounds useful as interfacial layer in polymer solar cells to enhance solar cell efficiency. Polymer solar cell including a fullerene surfactant-containing interfacial layer intermediate cathode and active layer.
Type:
Application
Filed:
December 5, 2012
Publication date:
June 27, 2013
Applicant:
University of Washington Through its Center for Commercialization
Inventor:
University of Washington Through Its Center for Commercialization
Abstract: Compounds of the general formulae (1) and (2) A-B-D-B?-A???(1) and A-B-D-E??(2) in which A and A? may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B? may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residu
Type:
Grant
Filed:
November 10, 2006
Date of Patent:
June 25, 2013
Assignee:
IMTM GmbH
Inventors:
Siegfried Ansorge, Klaus Neubert, Ute Bank, Irene Reichstein, Jürgen Faust, Michael Täger, Petra Fuchs, Bianca Senns