The Hetero Ring Contains Four Members Including Nitrogen And Carbon Patents (Class 548/950)
  • Patent number: 10383871
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: August 20, 2019
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Patent number: 9475800
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: October 25, 2016
    Assignee: VERNALIS (R&D) LTD.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Publication number: 20150148543
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Feng Li, Yihan Wang
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Patent number: 9024028
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: May 5, 2015
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Feng Li, Yihan Wang
  • Patent number: 9006227
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: April 14, 2015
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Publication number: 20150094470
    Abstract: Compounds and method of preparation of Si—X and Ge—X compounds (X?N, P, As and Sb) via dehydrogenative coupling between the corresponding unsubstituted silanes and amines (including ammonia) or phosphines catalyzed by metallic catalysts is described. This new approach is based on the catalytic dehydrogenative coupling of a Si—H and a X—H moiety to form a Si—X containing compound and hydrogen gas (X?N, P, As and Sb). The process can be catalyzed by transition metal heterogenous catalysts such as Ru(0) on carbon, Pd(0) on MgO) as well as transition metal organometallic complexes that act as homogeneous catalysts. The —Si—X products produced by dehydrogenative coupling are inherently halogen free. Said compounds can be useful for the deposition of thin films by chemical vapor deposition or atomic layer deposition of Si-containing films.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 2, 2015
    Inventors: Antonio Sanchez, Gennadily Itov, Peng Zhang, Matthew Damien Stephens
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8980877
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C1-C6 alkyl, optionally substituted by C3-C8 cycloalkyl, C6-C10 aryl or hetero(C2-C9)aryl; (CO)R2; (SO2)R3; C3-C8 cycloalkyl; C6-C10 aryl; or hetero(C2-C9)aryl; R1 is halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; Y is CH2 or NR4; Z is C?R5; and R2, R3, R4, and R5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: March 17, 2015
    Assignee: DAC S.R.L.
    Inventors: Mario Varasi, Florian Thaler, Raffaella Amici, Agnese Abate, Maria Carmela Fulco, Saverio Minucci, Ciro Mercurio
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Patent number: 8962835
    Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 24, 2015
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Publication number: 20150005286
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 1, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Johnny Y. Nagasawa, Andiliy G. Lai, Celine Bonnefous
  • Publication number: 20140371175
    Abstract: Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Michael Van Zandt, Adam Golebiowski, Min Koo Ji, Darren Whitehouse, Todd Ryder, Raymond Paul Beckett
  • Patent number: 8912188
    Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: December 16, 2014
    Assignee: BioEnergenix, LLC
    Inventors: John M. McCall, Donna L. Romero, Robert C. Kelly
  • Publication number: 20140349991
    Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 27, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 8895559
    Abstract: A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke
  • Patent number: 8877759
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: September 4, 2012
    Date of Patent: November 4, 2014
    Assignee: Vertex Pharnaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Publication number: 20140323462
    Abstract: Provided are compounds of Formula I, R1-L1-A-L2-R2??(I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Simona M. Ceccarelli, Carine Guerot, Henner Knust
  • Patent number: 8865715
    Abstract: The invention relates to compounds the formula (I): and pharmaceutically usable salts, tautomers and stereoisomers thereof, wherein R1, R2 and R3 are defined herein. The compounds of formula (I) and their pharmaceutically usable salts, tautomers and stereoisomers are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: October 21, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J. J. Mueller, Eugen Merkul
  • Publication number: 20140309206
    Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Publication number: 20140303384
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Inventors: Brian A. Duclos, Richard Andrew Ewin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Derek James Sheehan, Susan Mary Kult Sheehan, Donald James Skalitzky, Rajendran Vairagoundar
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Publication number: 20140303232
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
  • Patent number: 8853196
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: October 7, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
  • Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Publication number: 20140256654
    Abstract: A compound having the formula: wherein X is S, SO or SO2; one of R1, R2, and R3 is O and the others of R1, R2 and R3 are independently, the same or different, CH2, or CR13 wherein, R13 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)mOR15, wherein R15 is an alkyl group or an aryl group and m is an integer in the range of 1 to 10, and one of R5, R6, and R7 is O and the others of R5, R6 and R7 are independently, the same or different, CH2, or CR14 wherein, R14 is an alkyl group, an alkenyl group, an alkynyl group, a trialkylsilyl group, or —(CH2)nOR16, wherein R16 is an alkyl group or an aryl group and n is an integer in the range of 1 to 10; R4 and R8 are independently, the same or different, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, a heteroaryl group, a C1-C3 alkoxy group, an aryloxy group, or —(CH2)qOR17, wherein R17 is an alkyl group or an aryl group and q is an integer in the range of 1 to 10, provided that R4 is not a C1-C3 alkoxy g
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Joel S. Greenberger, Michael W. Epperly, Melissa M. Sprachman, Julie Pamela Goff
  • Patent number: 8822469
    Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Somhairle MacCormick, Pierre-Henri Storck, Michael Paul Mortimore, Jean-Damien Charrier, Ronald Knegtel, Stephen Clinton Young, Joanne Pinder, Steven John Durrant
  • Patent number: 8815926
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20140235872
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Application
    Filed: April 29, 2014
    Publication date: August 21, 2014
    Applicant: SIRNA THERAPEUTICS, INC.
    Inventors: Brian W. BUDZIK, Steven L. COLLETTI, Jennifer R. DAVIS, Ivory D. HILLS, Darla Danile SEIFRIED, Matthew G. STANTON
  • Publication number: 20140199600
    Abstract: The present invention provides a nonaqueous electrolyte solution, which can improve flame retardancy and ameliorate performances of a battery without deteriorating the basic battery performance as far as possible, and a secondary battery. The nonaqueous electrolyte solution is a nonaqueous electrolyte solution for a secondary battery that contains metal salts including ions of metals belonging to group 1 or 2 of the periodic table and a specific cyclic compound having phosphorus and nitrogen atoms in a non-protonic solvent. The non-protonic solvent is a solvent that contains at least one kind of carboxylic acid ester compound and carbonic acid ester compound, and a ratio (MPN/Ms) between a mass (Ms) of the non-protonic solvent containing the metal salts and a mass (MPN) of the cyclic compound is 0.01 to 1.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Toshihiko YAWATA, Ikuo KINOSHITA
  • Publication number: 20140179638
    Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
    Type: Application
    Filed: July 26, 2012
    Publication date: June 26, 2014
    Applicant: KBP BIOSCIENCES CO., LTD.
    Inventors: Hui Zhang, Yanyan Dong
  • Publication number: 20140179660
    Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: August 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Publication number: 20140171649
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Application
    Filed: January 26, 2012
    Publication date: June 19, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: Feng Li, Yihan Wang
  • Publication number: 20140171402
    Abstract: The present invention relates to an azetidine derivative or a pharmaceutically acceptable salt thereof, and an antidepressant agent or a composition for the prevention or treatment of psychiatric disorders including the same. The azetidine derivative is useful as a triple reuptake inhibitor capable of inhibiting reuptake of the neurotransmitters, dopamine, serotonin, and norepinephrine at the same time.
    Type: Application
    Filed: September 4, 2012
    Publication date: June 19, 2014
    Inventors: Hoh-Gyu Hahn, Kee-Dal Nam, Min-soo Han, Young-Hue Han, Chi-Man Song, Dong-Yun Shin
  • Patent number: 8742110
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: June 3, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu
  • Publication number: 20140128360
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: April 17, 2012
    Publication date: May 8, 2014
    Applicant: Integrative Research Laboratories Swenden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Publication number: 20140128361
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 8, 2014
    Applicants: Pharmacopeia Drug Discovery, Inc., Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X.H. Le, Jeffrey H. Lowrie, Kurt W. Salonz, Suresh D. Babu
  • Patent number: 8697888
    Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: April 15, 2014
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Yiu-Yin Cheung
  • Publication number: 20140094445
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140088077
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: December 3, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Publication number: 20140088079
    Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.
    Type: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Applicant: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Patent number: 8669252
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Patent number: 8658794
    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
  • Patent number: 8658646
    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
  • Publication number: 20140051678
    Abstract: The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other active agents. The present invention further relates to use of the compounds of the invention as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit. More particularly the present invention relates to the use of the compounds of the invention in a method of treating and/or preventing cancers presenting tumor-initiating cells.
    Type: Application
    Filed: November 24, 2011
    Publication date: February 20, 2014
    Applicant: STEMERGIE BIOTECHNOLOGY SA
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Riccardo Cribiu
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
  • Publication number: 20140018342
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 16, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee