Nitrogen Attached Directly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/190)
  • Patent number: 10213432
    Abstract: The present invention relates to a dosage regimen for a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a dosage regimen for the treatment of patients suffering from a proliferative disease, such as, for example, cancer, with a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: February 26, 2019
    Assignee: NOVARTIS AG
    Inventors: Samit Hirawat, Cristian Massacesi
  • Patent number: 9630929
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: April 25, 2017
    Assignee: XENON PHARMACEUTICALS INC.
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Patent number: 9447058
    Abstract: The present invention relates to 1,3-thiazole compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: September 20, 2016
    Assignees: Duke University, Chaperone Therapeutics, Inc.
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • Patent number: 9303024
    Abstract: This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: April 5, 2016
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Evripidis Gavathiotis
  • Patent number: 9150561
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: October 6, 2015
    Assignee: MERCK SERONO S.A.
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Patent number: 9067922
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes, and to methods of treatment, wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: June 30, 2015
    Assignee: Pfizer Limited
    Inventors: Robert Ian Storer, Nigel Alan Swain, Robert McKenzie Owen
  • Patent number: 8940271
    Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: January 27, 2015
    Assignee: Abbott Laboratories
    Inventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
  • Patent number: 8937065
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: January 20, 2015
    Assignee: Clevexel Pharma
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Patent number: 8889722
    Abstract: An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be orally administered is provided. Disclosed is a pharmaceutical composition containing, as an active ingredient, an optically active compound represented by the formula: wherein, R1 is a halogen atom or C1-C3 alkyloxy; R2 is C1-C8 alkyl; R3 is C1-C8 alkyl; R4 and R5 are each independently a fluorine atom or chlorine atom; R6 is C1-C3 alkyl or C1-C3 alkyloxy; * indicates that a carbon atom marked with an asterisk is an asymmetric carbon, a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: November 18, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masami Takayama, Noriyuki Kurose
  • Patent number: 8871944
    Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: October 28, 2014
    Assignee: Gifu University
    Inventor: Toshiaki Murai
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8846730
    Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: September 30, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
  • Patent number: 8841334
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: September 23, 2014
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson, Xueqing Wang
  • Publication number: 20140249154
    Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • Publication number: 20140239229
    Abstract: An organic electroluminescence (EL) device comprising an organic EL material represented by the following Formula (1):
    Type: Application
    Filed: February 25, 2014
    Publication date: August 28, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Nobutaka AKASHI, Toshiaki MURAI
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Patent number: 8815923
    Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: August 26, 2014
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
  • Publication number: 20140221658
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Applicant: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Patent number: 8716323
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8691854
    Abstract: The present invention relates to the field of pharmacy, especially the treatment of neurodegenerative diseases. The invention specifically relates to a family of chemical compounds for which a neuroprotective activity has been demonstrated. Given that certain members of said family are novel compounds which have never been described, the invention relates to said novel products, the synthesis method thereof and certain novel intermediate synthesis products. The present invention further relates to compositions comprising the compounds of said family, and the use of said compounds as medicaments, especially for the preparation of a medicament for the treatment of neurodegenerative diseases.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: April 8, 2014
    Assignee: Trophos
    Inventors: Corinne Chaimbault, Cyrille Drouot, Laure Jamot, Rebecca Pruss, Céline Simon
  • Patent number: 8653259
    Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: February 18, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang
  • Patent number: 8642278
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: February 4, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Patent number: 8624036
    Abstract: The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: January 7, 2014
    Assignee: Dompe S.p.A.
    Inventors: Marcello Allegretti, Andrea Aramini, Gianluca Bianchini, Maria Candida Cesta
  • Publication number: 20140005190
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Application
    Filed: June 27, 2013
    Publication date: January 2, 2014
    Applicants: Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.
    Inventors: JONATHAN BAYLDON BAELL, CHINH THIEN BUI, PETER COLMAN, DANETTE A. DUDLEY, WAYNE J. FAIRBROTHER, JOHN A. FLYGARE, GUILLAUME LAURENT LESSENE, CHUDI NDUBAKU, GEORGE NIKOLAKOPOULOS, CARL STEVEN RYE, BRAD EDMUND SLEEBS, BRIAN JOHN SMITH, KEITH GEOFFREY WATSON, STEVEN W. ELMORE, ANDREW M. PETROS, ANDREW J. SOUERS, PETER CZABOTAR
  • Patent number: 8614229
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Patent number: 8580710
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one aminothiazoline compound I of formula I: wherein variables R1, R2, R3, R4, R5, and R6 are as defined in the description of the application and 2) at least one active compound II selected from group A as defined in the description, use of these mixtures for combating insects, acarids, or nematodes, and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites using these mixtures.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: November 12, 2013
    Assignee: BASF SE
    Inventors: Markus Kordes, Ronan Le Vezouet, Jürgen Langewald, Ralph Paulini, Deborah L. Culbertson, Douglas D. Anspaugh, Luiz Antonio Jose, Faraneh Oloumi
  • Patent number: 8568756
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8541588
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Grant
    Filed: February 20, 2012
    Date of Patent: September 24, 2013
    Assignees: Pfizer Limited, Icagen, Inc.
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Patent number: 8530668
    Abstract: An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be orally administered is provided. Disclosed is a pharmaceutical composition containing, as an active ingredient, an optically active compound represented by the formula: wherein, R1 is a halogen atom or C1-C3 alkyloxy; R2 is C1-C8 alkyl; R3 is C1-C8 alkyl; R4 and R5 are each independently a fluorine atom or chlorine atom; R6 is C1-C3 alkyl or C1-C3 alkyloxy; * indicates that a carbon atom marked with an asterisk is an asymmetric carbon, a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: July 29, 2008
    Date of Patent: September 10, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masami Takayama, Noriyuki Kurose
  • Patent number: 8524753
    Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.
    Type: Grant
    Filed: January 31, 2012
    Date of Patent: September 3, 2013
    Assignee: AbbVie Inc.
    Inventors: Dale J. Kempf, Charles A. Flentge, John T. Randolph, Peggy Huang, Larry L. Klein
  • Patent number: 8524750
    Abstract: A compound of Formula (I) wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: September 3, 2013
    Assignee: Glaxo Group Limited
    Inventors: Lluis Ballell Pages, Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Maria Luisa Leon Diaz, Alfonso Mendoza Losana, Matthew James Wolfendale
  • Patent number: 8524718
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: September 3, 2013
    Assignee: Addex Pharma S.A.
    Inventors: Christelle Boléa, Sylvain Celanire
  • Patent number: 8492415
    Abstract: The present invention relates to novel heterocyclic compounds, including oxadiazole compounds, pharmaceutical compositions and their use in the inhibition of reverse transcriptase and the treatment of HIV (1 and 2) infections, AIDS and ARC and other viral infections.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: July 23, 2013
    Assignee: Yale University
    Inventor: William L. Jorgensen
  • Publication number: 20130184315
    Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: July 18, 2011
    Publication date: July 18, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbH
    Inventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
  • Publication number: 20130143927
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 6, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Patent number: 8431604
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Grant
    Filed: February 15, 2005
    Date of Patent: April 30, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling
  • Patent number: 8426433
    Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: April 23, 2013
    Assignee: Obschestvo S Ogranichennoi Otvetsttvennoctiyu “Bionika”
    Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
  • Patent number: 8426454
    Abstract: Disclosed herein is a compound having a structure compositions, methods, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: April 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Todd M. Heidelbaugh, Daniel W. Gil, Ken Chow, Michael E. Garst
  • Patent number: 8410152
    Abstract: Described are compounds having a thiazolhydrazide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said thiazolhydrazide compounds can be used for prophylaxis and/or treatment of neurodegenerative diseases and conditions.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: April 2, 2013
    Assignees: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e. V., Technische Universitat Darmstadt, The Provost Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth near Dublin
    Inventors: Eckhard Mandelkow, Eva-Maria Mandelkow, Markus Pickhardt, Jacek Biernat, David George Lloyd, Boris Schmidt, Gregor Larbig
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 8362267
    Abstract: Disclosed are a novel thiazole-containing benzophenone derivative represented by formula 1, and an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof, a pharmaceutical composition comprising the derivative, a use of the derivative as therapeutic agent and a method for preparing the derivative. The benzophenone thiazole derivatives inhibit formation of microtubules and eliminate actively proliferating cells of malignant tumors to control general cell proliferation. In formula 1, R, R1 and R2 are defined as above.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: January 29, 2013
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Nam-Song Choi, Young-Hoon Kim, Jae-Kwang Lee, Hee-Ryong Kang, Ho-Jin Choi, Seung-Kee Moon, Soo-Jin Kim, Gyu-Tae Park, Byeong-Hoon Han, Dal-Hyun Kim, Jae-Hoon Choi, Sung-Sook Lee, Soon-Kil Ahn, Kyung-Joo Lee, Su-Yeal Bae
  • Patent number: 8362050
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by G protein-coupled receptors, in particular G protein-coupled receptor 120.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: January 29, 2013
    Assignee: IRM LLC
    Inventors: Xiaohui He, Xuefeng Zhu, Kunyong Yang, Robert Epple, Hong Liu
  • Patent number: 8357711
    Abstract: The invention is directed to compounds of the formula in which R5, R6 B and Z are defined supra.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: January 22, 2013
    Assignees: Pfizer Limited, Icagen, Inc.
    Inventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
  • Publication number: 20120329811
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 27, 2012
    Inventors: Christelle Boléa, Sylvain Celanire
  • Patent number: 8314249
    Abstract: The present invention is a process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine as set forth in formula (I) and new intermediates of the preparation process.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: November 20, 2012
    Assignee: Sanofi
    Inventors: Janos Fazekas, Peter Miskolczi, Annamaria Molnar, Bela Agai, Zsolt Parkanyi
  • Patent number: 8309739
    Abstract: The use of a compound of formula I wherein X is (i), (ii) or (iii) Y is O, S(O)m, NR3, CR5R6, CR5R6—CR7R8, O—CR7R8, S(O)m—CR7R8, NR3—CR7R8, CR5R6—O, CR5R6—S(O)m, CR5R6—NR3, SO2—NR3, NR3—SO2, NR3—O or O—NR3; m is 0, 1, or 2; the ring (T) is a 5- or 6-membered aromatic or heteroaromatic ring; R1 to R10 are specified organic groups and n and is 0, 1, 2, 3 or 4; or salts or N-oxides thereof or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: November 13, 2012
    Assignee: Syngenta Limited
    Inventors: Anthony Cornelius O'Sullivan, Juergen Harry Schaetzer, Christoph Luethy, Allison Clare Elliott, Christopher John Mathews
  • 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: 8236835
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: August 7, 2012
    Assignees: Novartis AG, Xenon Pharmaceuticals Inc.
    Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov