The Nitrogen Is In A Substituent Attached To The Ring Nitrogen Of The Five Membered Hetero Ring Patents (Class 548/569)
  • Patent number: 10035762
    Abstract: The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: July 31, 2018
    Assignee: ExxonMobil Chemical Patents Inc.
    Inventors: Kirk D. Schmitt, Stephen Zushma, Allen W. Burton
  • Patent number: 9540325
    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: Grant
    Filed: August 8, 2012
    Date of Patent: January 10, 2017
    Assignee: Immunomet Therapeutics, Inc.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 8961959
    Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: February 24, 2015
    Assignee: The Regents of the University of Michigan
    Inventors: Scott Larsen, Akira Abe, Liming Shu, Michael William Wilson, Richard F. Keep, James A. Shayman
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8779163
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: July 15, 2014
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20140179661
    Abstract: A N1-cyclic amine-N5-substituted 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: April 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: 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
  • Patent number: 8759541
    Abstract: The current application relates to a metal catalyst of formula (I): M[ADC][X]n, wherein M is a metal, ADC is a chiral acyclic diaminocarbene ligand, and X is a neutral or anionic ligand. The ADC ligand is prepared from the corresponding chiral formamidium salt precursor. The metal catalyst is used for asymmetric organic synthesis reactions such as hydrosilations, hydrogenations, conjugate additions, and cross-couplings.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: June 24, 2014
    Inventors: Avinash N. Thadani, Rukundo Ntaganda, Mira M. Beshai
  • Publication number: 20140128335
    Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 8, 2014
    Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20130157851
    Abstract: New phenylamidines are described, having general formula (I): and their use for the control of phytopathogenic fungi.
    Type: Application
    Filed: August 18, 2011
    Publication date: June 20, 2013
    Applicant: ISAGRO S.P.A.
    Inventors: Marilena Gusmeroli, Lucio Filippini, Franco Pellacini, Paolo Bravini, Alexia Elmini, Matteo Santino Vazzola, Christian Badaracco
  • Publication number: 20130095089
    Abstract: Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 18, 2013
    Applicant: The Regents of The University of Michigan
    Inventor: The Regents of The University of Michigan
  • Publication number: 20130072488
    Abstract: Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
    Type: Application
    Filed: May 13, 2011
    Publication date: March 21, 2013
    Applicant: Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Yongyong Zheng, Yunfeng Liao, Yali Li
  • Publication number: 20130023563
    Abstract: Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoaniline derivative represented by the following formula (1-1) or a pharmaceutically acceptable salt thereof: <in the formula (1-1), each symbol is as defined in the Description>, and a pharmaceutical composition containing the amidinoaniline derivative or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 24, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC.
  • Publication number: 20120296088
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Application
    Filed: March 14, 2012
    Publication date: November 22, 2012
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20120190854
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Patent number: 8106090
    Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: January 31, 2012
    Assignee: Eli Lilly and Company
    Inventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Michael Robert Wiley
  • Publication number: 20120022271
    Abstract: [Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate.
    Type: Application
    Filed: April 13, 2010
    Publication date: January 26, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Atsushi Ohigashi, Takashi Kikuchi
  • Publication number: 20120004225
    Abstract: The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
    Type: Application
    Filed: January 22, 2010
    Publication date: January 5, 2012
    Applicant: NeuroTherapeutics Pharma, Inc.
    Inventors: Stephen Wanaski, John J. Partridge, Stephen D. Collins
  • Publication number: 20110300567
    Abstract: A method for identifying the redox activity of a subject compound is disclosed. The method can be performed aerobically and can include forming a mixture comprising a free-radical precursor and a compound to be tested, and converting the free-radical precursor into a free-radical anion and a free-radical cation. After the free radical cation and the free radical anion have been formed, the relative redox activity of the subject compound may cause a difference in the rate of photo-bleaching of the mixture and/or the rate of superoxide generation. These differences can be quantified and used to identify the redox activity of the subject compound. This sensitive technique for measuring redox activity can be used to screen compounds for various biological applications. Drugs also can be developed based on the relationship between redox activity and biological activity for particular biological applications.
    Type: Application
    Filed: August 9, 2011
    Publication date: December 8, 2011
    Inventors: Jonathan J. Abramson, Benjamin S. Marinov
  • Publication number: 20110098392
    Abstract: The present invention relates to an organopolysiloxane composition that can be vulcanized at room temperature into an elastomer that is crosslinked by polycondensation and that does not contain alkyltin-based catalysts which exhibit toxicity problems. The invention also relates to novel polycondensation catalysts having a guanidine structure, in silicone chemistry, and to the uses thereof as catalysts for the organopolysiloxane polycondensation reaction.
    Type: Application
    Filed: March 24, 2009
    Publication date: April 28, 2011
    Applicant: BLUESTAR SILICONES FRANCE
    Inventors: Georges Barrandon, Delphine Blanc, Christian Maliverney, Hervé Parisot
  • Publication number: 20100197640
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Application
    Filed: January 29, 2010
    Publication date: August 5, 2010
    Applicant: 4SC AG
    Inventor: Stefano PEGORARO
  • Patent number: 7763738
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: July 27, 2010
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Publication number: 20100184996
    Abstract: A process for the formation of 2-(methyloxy)-N-[2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]-4,6-bis(trifluoromethyl)benzamide is disclosed, comprising treatment of 2,4-ditrifluoromethyl-6-methoxy-benzoic acid with an arylsulphonyl halide, C1-6alkylsulphonyl halide or di-C1-6alkylphosphoryl chloride, in the presence of a base and an aprotic solvent; followed by reaction with [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine or a salt thereof. Also disclosed is a process for the formation of [2-methyl-1-phenyl-2-(1-pyrrolidinyl)propyl]amine comprising: i) treatment of an ?-haloketone with an alcohol in the presence of a base followed by reaction with pyrrolidine; ii) treatment of the product of stage i) with Ar—CH(R5)N H2 wherein R5 is C1-4alkyl and Ar is optionally substituted phenyl, followed by reduction with a sodium borohydride derivative; and iii) reduction of the product of stage ii) with hydrogen and a palladium catalyst.
    Type: Application
    Filed: June 18, 2008
    Publication date: July 22, 2010
    Applicant: GLAXO GROUP LIMITED
    Inventors: Alcide Perboni, Nicola Giubellina
  • Publication number: 20100158818
    Abstract: The present application relates to N-chlorinated cationic compounds of Formula I or a salt thereof, and associated compositions and methods of use as antimicrobial agents.
    Type: Application
    Filed: November 6, 2009
    Publication date: June 24, 2010
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Satheesh K. Nair
  • Publication number: 20100120615
    Abstract: The present invention relates to 4-cycloalkyl- or 4-aryl-substituted phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.
    Type: Application
    Filed: March 8, 2008
    Publication date: May 13, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Klaus Kunz, Ralf Dunkel, Jörg Nico Greul, Oliver Guth, Kerstin Ilg, Darren James Mansfield, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann, Arnd Voerste, Jean-Pierre Vors
  • Publication number: 20100010216
    Abstract: The invention provides a 2-fluorinated acyl-3-aminoacrylonitrile derivative, and a method for producing the same. A desired 2-fluorinated acyl-3-aminoacrylonitrile derivative represented by the following Formula (3) is obtained by reacting a fluorinated acyl derivative with an aminoacrylonitrile derivative. In Formula (3), Rf represents an alkyl group having 1 to 6 carbon atoms which is substituted with at least one fluorine atom, R1 and R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like, and R3 represents an alkyl group having 1 to 6 carbon atoms or the like.
    Type: Application
    Filed: December 18, 2007
    Publication date: January 14, 2010
    Applicant: Mitsui Chemicals Agro, INC
    Inventors: Hideki Umetani, Yoji Aoki, Takeshi Kakimoto
  • Publication number: 20090197918
    Abstract: The present invention relates to benzyloxy- and phenethyl-substituted phenyl-amidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: September 12, 2006
    Publication date: August 6, 2009
    Applicant: Bayer CropScience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Olga Malsam, Eva Maria Franken
  • Patent number: 7560569
    Abstract: Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically acceptable salts thereof are also included (Example: (2S,4S)-1-[[(4-carbamoylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile)).
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: July 14, 2009
    Assignee: Kyorin Pharmaceutical Co., Ltd
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Satoru Katayama, Taku Shibue, Koji Murakami, Tomohiro Ide
  • Publication number: 20090176773
    Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.
    Type: Application
    Filed: May 18, 2006
    Publication date: July 9, 2009
    Applicant: FORSCHUNGSVERBUND BERLIN E.V.
    Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
  • Patent number: 7557215
    Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6, R7 and R8 is selected from X2, and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: July 7, 2009
    Assignee: Somanta Limited
    Inventors: Laurence Hylton Patterson, Klaus Pors, Paul Henry Teesdale-Spittle
  • Publication number: 20090131433
    Abstract: This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-i
    Type: Application
    Filed: June 12, 2006
    Publication date: May 21, 2009
    Applicant: PFIZER INC.
    Inventor: Travis T. Wager
  • Patent number: 7528156
    Abstract: The invention provides compounds of general formula (D wherein m, n, Q, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: November 22, 2004
    Date of Patent: May 5, 2009
    Assignee: AstraZeneca AB
    Inventors: Tomas Eriksson, Tomas Klingstedt, Tesfaledet Mussie
  • Publication number: 20090080074
    Abstract: A polymer film includes: a wavelength dispersion regulator represented by formula (I): wherein R1 and R2 each independently represents a hydrogen atom, an alkyl group or an aryl group, provided that both R1 and R2 are not hydrogen atoms at the same time; and R3 and R4 each independently represents an electron-withdrawing substituent, and R1 and R2, or R3 and R4 may be bonded together to form a ring, and wherein the polymer film has a retardation value that satisfies the following formulae (1) and (2): 70 nm?Rth(548)?300 nm??Formula (1) Rth(628)<Rth(548)<Rth(446)??Formula (2) wherein Rth(?) represents a retardation value expressed in nm in a film thickness direction measured at a wavelength of ? nm.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 26, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Nobutaka Fukagawa, Masaki Noro, Teruki Niori
  • Patent number: 7423059
    Abstract: The present invention relates to certain imine-substituted heterocyclic compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
    Type: Grant
    Filed: June 28, 2004
    Date of Patent: September 9, 2008
    Assignee: Wyeth
    Inventors: Graham J. Durant, Michael Maillard, Jun Qing Guo
  • Publication number: 20080207735
    Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
    Type: Application
    Filed: July 14, 2006
    Publication date: August 28, 2008
    Inventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Michael Robert Wiley
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7365070
    Abstract: This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: wherein X is oxygen or sulfur; G is G1 or G2: L1, L2, L3 and Q are linker groups, and Rings A, B and C, and R1-R14 are described in the specification. The compounds are antagonists of melanocortin receptors.
    Type: Grant
    Filed: December 4, 2003
    Date of Patent: April 29, 2008
    Assignee: Ore Pharmaceuticals Inc.
    Inventors: Tricia J. Vos, Michael Patane, Michael E. Solomon, Christopher Blackburn, Mihaela D. Danca
  • Patent number: 7351825
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: April 1, 2008
    Assignee: Japan Tobacco Inc.
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Patent number: 7288566
    Abstract: An N-hydroxyformamidine compound of the following formula or a pharmaceutically acceptable salt thereof: wherein R1, A and R are as defined herein. The compounds inhibit 20-HETE-producing enzymes, 20-HETE being involved in the effects of causing microvascular constriction or dilation in major organs (e.g., kidneys, cerebral blood vessels) or of inducing cell proliferation.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: October 30, 2007
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Hiroyuki Kakinuma, Hideaki Amada
  • Patent number: 7265228
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: September 4, 2007
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Patent number: 7256191
    Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.
    Type: Grant
    Filed: August 31, 2004
    Date of Patent: August 14, 2007
    Assignee: Aryx Therapeutics
    Inventor: Pascal Druzgala
  • Patent number: 7026485
    Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: April 11, 2006
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Kathryn L. Reed, Ko-Chung Lin, John Nicholas Freskos, Michael Clare, Donald Joseph Rogier, Jr., Robert M. Heintz, Michael L. Vazquez, Richard A. Mueller
  • Patent number: 6919368
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: July 19, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Ui Tae Kim, Dean A. Wacker, Changsheng Zheng
  • Patent number: 6900243
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 31, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
  • Patent number: 6887872
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: May 3, 2005
    Assignee: N-Gene Research Laboratiories Inc.
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs