Chalcogen Bonded Directly To Ring Carbon Of The Oxadiazole Ring Patents (Class 548/144)
  • Patent number: 9102635
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein X is defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: August 11, 2015
    Assignee: NOVARTIS AG
    Inventors: David Weninger Barnes, Dean Franklin Rigel
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Patent number: 9000016
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: April 7, 2015
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Patent number: 8987473
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Sato Pharmaceutical Co., Ltd.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Publication number: 20150018543
    Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: April 28, 2014
    Publication date: January 15, 2015
    Applicants: Institut Pasteur Korea, INSERM (Institut National de la Sante et de la Recherche Medicale)
    Inventors: Priscille BRODIN, Thierry CHRISTOPHE, Zaesung NO, Jaeseung KIM, Auguste GENOVESIO, Denis Philippe Cedric FENISTEIN, Heekyoung JEON, Fanny Anne EWANN, Sunhee KANG, Saeyeon LEE, Min Jung SEO, Eunjung PARK, Monica CONTRERAS DOMINGUEZ, Ji Youn NAM, Eun Hye KIM
  • Publication number: 20140378493
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Patent number: 8846729
    Abstract: The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: September 30, 2014
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140274690
    Abstract: Provided herein are new 3,5-disubstituted-1,3,4-oxadiazol-2(3H)-ones and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Monsanto Technology LLC
    Inventors: Urszula J. Slomczynska, Matthew W. Dimmic, William P. Haakenson, JR., Al S. Wideman
  • Publication number: 20140235660
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
  • Publication number: 20140228365
    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: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Publication number: 20140228415
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein X is defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Dean Franklin RIGEL
  • Patent number: 8802861
    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: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Publication number: 20140135291
    Abstract: The present invention relates to novel 2-thio-1,3,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140135365
    Abstract: The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 7, 2013
    Publication date: May 15, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140128348
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140128366
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Patent number: 8629283
    Abstract: The present invention relates to compounds that modulate the replication of negative-sense, single-stranded RNA viruses, such as influenza virus, and the use of such compounds. The invention relates to methods for increasing the titer of negative-sense, single-stranded RNA viruses, such as influenza virus, in substrates for virus propagation (e.g., tissue culture). The invention also relates to the use of compounds that decrease virus replication as antiviral agents. The invention further relates to methods for identifying compounds that modulate the replication of negative-sense, single-stranded RNA viruses, in particular, influenza virus.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: January 14, 2014
    Assignee: Icahn School of Medicine at Mount Sinai
    Inventors: Megan L. Shaw, Hans-Heinrich Hoffmann, Adolfo Garcia-Sastre, Peter Palese
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Patent number: 8618145
    Abstract: The invention provides small molecule compounds capable of accelerating proliferation of stem cells and uses thereof. The compounds play an important role in the research of stem cell proliferation mechanism. The invention further relates to the uses of the compounds and relevant compounds thereof in the preparation of stem cell proliferation accelerators and the preparation of medicines accelerating stem cell proliferation. The invention also relates to the uses of the compounds in the preparation of medicines for the treatment of various diseases arising from functional cells loss or damage. The diseases arising from stem cell trauma comprise diseases related to the degeneration or damage of nervous system cells, blood system diseases, diseases related to the loss or damage of cardiovascular cells, skin burn and the like.
    Type: Grant
    Filed: May 12, 2009
    Date of Patent: December 31, 2013
    Inventors: Mei Han, Yan Feng, Yuanyuan Sun
  • Publication number: 20130324409
    Abstract: The present invention provides methods of regulating plant stress tolerance.
    Type: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Inventors: SEAN R. CUTLER, ANDREW DEFRIES
  • Publication number: 20130303515
    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
  • Publication number: 20130289003
    Abstract: A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.
    Type: Application
    Filed: October 25, 2011
    Publication date: October 31, 2013
    Inventors: Amjad Ali, Michael Man-Chu Lo, Robert K. Baker, Zhiqiang Guo, Brent Whitehead, Timothy J. Henderson, Edward Metzger, Lin Yan, Shrenik K. Shah, James Dellureficio, Jun Wang
  • Patent number: 8513235
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: August 20, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • Patent number: 8492378
    Abstract: For the purpose of providing a GSK-3? inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3?-related pathology or disease, the present invention provides a GSK-3? inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: July 23, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Fumio Itoh, Jun Kunitomo, Hiromi Kobayashi, Eiji Kimura, Morihisa Saitoh, Tomohiro Kawamoto, Hiroki Iwashita, Katsuhito Murase
  • Publication number: 20130109649
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: October 25, 2012
    Publication date: May 2, 2013
    Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
  • Patent number: 8378118
    Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: February 19, 2013
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
  • Patent number: 8357705
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain or other conditions.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: January 22, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Saskia Zemolka, Bert Nolte, Klaus Linz, Derek John Saunders, Wolfgang Schröder, Werner Englberger, Fritz Theil, Hans Schick, Jens Kaufmann, Julian Gebauer, Helmut Sonnenschein
  • Publication number: 20120309769
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: June 6, 2012
    Publication date: December 6, 2012
    Applicant: SCRIPPS RESEARCH INSTITUTE, THE
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
  • Patent number: 8299264
    Abstract: A compound represented by the formula (1): wherein Ar represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, Ar? represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, and R represents an alkyl group having 1 to 4 carbon atoms.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: October 30, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Koji Hagiya, Yasutaka Aoyagi
  • Publication number: 20120232070
    Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.
    Type: Application
    Filed: March 9, 2012
    Publication date: September 13, 2012
    Applicant: Laboratoires Fournier SA
    Inventors: Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
  • Publication number: 20120202816
    Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Application
    Filed: January 10, 2012
    Publication date: August 9, 2012
    Applicant: Torrent Pharmaceuticals, Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
  • Publication number: 20120115894
    Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: February 22, 2010
    Publication date: May 10, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
  • Patent number: 8143424
    Abstract: A novel thyroid like compounds of formula (I), wherein R1, R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition and use thereof. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions including obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: March 27, 2012
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, Chaitanya Dutt, Vijay Chauthaiwale
  • Publication number: 20120065196
    Abstract: The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.
    Type: Application
    Filed: July 20, 2007
    Publication date: March 15, 2012
    Inventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Yoshihisa Nakada
  • Publication number: 20120053214
    Abstract: The invention provides small molecule compounds capable of accelerating proliferation of stem cells and uses thereof. The compounds play an important role in the research of stem cell proliferation mechanism. The invention further relates to the uses of the compounds and relevant compounds thereof in the preparation of stem cell proliferation accelerators and the preparation of medicines accelerating stem cell proliferation. The invention also relates to the uses of the compounds in the preparation of medicines for the treatment of various diseases arising from functional cells loss or damage. The diseases arising from stem cell trauma comprise diseases related to the degeneration or damage of nervous system cells, blood system diseases, diseases related to the loss or damage of cardiovascular cells, skin burn and the like.
    Type: Application
    Filed: May 12, 2009
    Publication date: March 1, 2012
    Inventors: Mei Han, Yan Feng, Yuanyuan Sun
  • Publication number: 20120029192
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Publication number: 20120022083
    Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.
    Type: Application
    Filed: February 9, 2011
    Publication date: January 26, 2012
    Applicant: ADHEREX TECHNOLOGIES, INC.
    Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
  • Publication number: 20120020881
    Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: December 4, 2009
    Publication date: January 26, 2012
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
  • Publication number: 20110207936
    Abstract: A compound represented by the formula (1): wherein Ar represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, Ar? represents an aromatic hydrocarbon group having 6 to 20 carbon atoms which may have a substituent, and R represents an alkyl group having 1 to 4 carbon atoms.
    Type: Application
    Filed: October 19, 2009
    Publication date: August 25, 2011
    Inventors: Koji Hagiya, Yasutaka Aoyagi
  • Patent number: 7977671
    Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: July 12, 2011
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
  • Patent number: 7943645
    Abstract: This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Grant
    Filed: July 8, 2008
    Date of Patent: May 17, 2011
    Assignee: SmithKline Beecham Limited
    Inventors: Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, Riccardo Novelli, Roderick Alan Porter
  • Patent number: 7906652
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH).
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: March 15, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert K. Baker, Jeffrey J. Hale, Shouwu Miao, Kathleen M. Rupprecht
  • Publication number: 20110034440
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Application
    Filed: April 10, 2009
    Publication date: February 10, 2011
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • Publication number: 20110034450
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: April 6, 2009
    Publication date: February 10, 2011
    Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFT
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Patent number: 7872032
    Abstract: The present invention is directed to 1,3,4-oxadiazalones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: January 18, 2011
    Assignees: Aventis Parmaceuticals Inc., Sanofi-Aventis Deutschland GmbH
    Inventors: Daniel G. McGarry, Jochen Goerlitzer, Stefanie Keil, Karen Chandross, Jean Merrill, Wolfgang Wendler
  • Patent number: 7863302
    Abstract: Compounds of formula and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: January 4, 2011
    Assignee: Eli Lilly and Company
    Inventors: Michael Gregory Bell, Michael James Genin, Peter Ambrose Lander, Lindsay Scott Stelzer, Robert Anthony Doti, Francisco Javier Agejas-Chicharro, Ana Belen Bueno Melendo, Peter Rudolph Manninen, Jason Matthew Ochoada, Quanrong Shen, Alan M. Warshawsky, Tianwei Ma, Ryan Edward Stites
  • Patent number: 7851493
    Abstract: The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist activity. What are described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: December 14, 2010
    Assignee: Sanofi-Aventis
    Inventors: Patrick Bernardelli, Stefanie Keil, Matthias Urmann, Hans Matter, Wolfgang Wendler, Maike Glien, Karen Chandross, Lan Lee, Corinne Terrier, Herve Minoux
  • Publication number: 20100305131
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 27, 2010
    Publication date: December 2, 2010
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20100292282
    Abstract: The present invention relates to a process for producing crystalline 3-[(1S)-1-(1-{(S)-(4-chlorophenyl)[3-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl]methyl}azetidin-3-yl)-2-fluoro-2-methyl-propyl]-5-fluorobenzonitrile, and novel salts, solvates, hydrates and polymorphs thereof.
    Type: Application
    Filed: October 20, 2008
    Publication date: November 18, 2010
    Inventors: Kevin R. Campos, Cheng-Yi Chen, Jennifer R. Foley, Michael Hillier, Wendy S. Jen, Amude M. Kassim, Artis Klapars, Andrey V. Peresypkin, Thorsten Rosner, Cecile G. Savarin, Matthew Tudge, Narayan Variankaval, Vicky Vydra, Dalian Zhao