Polycyclo Ring System Patents (Class 564/456)
  • Patent number: 9000047
    Abstract: The present invention relates to a compound of formula (I) for use as a medicine, in particular for use in the treatment of diseases mediated by the actvation of the protein kinase Erk1/2, such as neurogenerative illnesses like Alzheimer's and related dementia, epilepsy, Parkinson's disease, Huntington's disease, or stroke, and likewise relates to the pharmaceutical compositions containing said compound. The compound of formula (I) effectively inhibits the activation of the enzyme Erk1/2 induced by the tissue plasminogen activator (TPA) and also effectively inhibits the apoptosis generated by the ?-amyloid peptide.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: April 7, 2015
    Assignee: Farmalider, S.A.
    Inventors: Pilar Navarro Medrano, Elisabet Gregori Puigjane, Marisol Montolio Del Olmo, Ana Jimenez Redondo, Jordi Mestres Lopez
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Publication number: 20130303805
    Abstract: The present invention relates to a process for producing an amino compound by subjecting a polyamine and an alkenyl compound to addition reaction in the presence of an alkali metal hydride compound which is capable of supplying the amino compound in a stable manner without occurrence of odor.
    Type: Application
    Filed: January 16, 2012
    Publication date: November 14, 2013
    Applicant: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Hisayuki Kuwahara, Tomotaka Wada
  • Publication number: 20130072553
    Abstract: This invention relates to the drugs, derivatives and analogs containing adamantane structures of new indication applications of anti-tumor. The invention also relates to above compounds to treat tumors and other diseases with FIG. 1. These drugs, derivatives and analogs are generated by the modification of the parent or fragment structures and formation of pharmaceutically acceptable salts, complex salts or prodrug. The drugs, derivatives and analogs as described are administered alone or together with at least one known anti-tumor and immune chemotherapeutic agent including treatment of viral, bacterial and fungal diseases, neurological diseases, endocrine system diseases, and immune system diseases.
    Type: Application
    Filed: December 25, 2009
    Publication date: March 21, 2013
    Inventor: Lifeng Xu
  • Publication number: 20130065966
    Abstract: The present invention relates to a compound of formula (I) for use as a medicine, in particular for use in the treatment of diseases mediated by the actvation of the protein kinase Erk1/2, such as neurogenerative illnesses like Alzheimer's and related dementia, epilepsy, Parkinson's disease, Huntington's disease, or stroke, and likewise relates to the pharmaceutical compositions containing said compound. The compound of formula (I) effectively inhibits the activation of the enzyme Erk1/2 induced by the tissue plasminogen activator (TPA) and also effectively inhibits the apoptosis generated by the ?-amyloid peptide.
    Type: Application
    Filed: May 24, 2010
    Publication date: March 14, 2013
    Applicant: FARMALIDER, S.A.
    Inventors: Pilar Navarro Medrano, Elisabet Gregori Puigjane, Marisol Montolio Del Olmo, Ana Jimenez Redondo, Jordi Mestres Lopez
  • Publication number: 20120310022
    Abstract: The present invention relates to a composition and method for inhibiting the formation of naphthenate solids in a liquid hydrocarbon. The method includes contacting a composition including a rosin amine having a formula (I): or (II): where formula (AA): represents a single or double bond; R1, R2 and R5 each independently represent H, alkyl, alkenyl or an alkynyl group each having between one and ten carbon atoms, —(R3O)nR4 wherein R3 is an alkyl group having 1 to 3 carbon atoms and R4 is H, alkyl, alkenyl or an alkynyl group each having between one and ten carbon atoms; n is an integer between 5 and 50; X is a halide, sulphate, phosphate or acetate ion; and a demulsifier intermediate with the liquid hydrocarbon.
    Type: Application
    Filed: November 25, 2010
    Publication date: December 6, 2012
    Inventors: Chandrashekhar Khandekar, Suguna Gopal, James Smith
  • Publication number: 20120052019
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Application
    Filed: August 22, 2011
    Publication date: March 1, 2012
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20120028957
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 1, 2010
    Publication date: February 2, 2012
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8053603
    Abstract: The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: November 8, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott Christopher Malcolm, Michael Charles Hewitt, Larry R. Bush, Mark A. Varney, Una Campbell, Sharon Rae Engel, Larry Wendell Hardy, Patrick Koch, Jianguo Ma
  • Patent number: 7981930
    Abstract: Kits comprising an M2 inhibitor selected from amantadine and rimantadine; ribavirin, and a neuraminidase inhibitor (NAi) in an amount that is antivirally effective in the combination, an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin and a neuraminidase inhibitor are provided for the treatment of influenza. Some embodiments of the kits comprise an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin, and a neuraminidase inhibitor.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: July 19, 2011
    Assignee: Adamas Pharmaceuticals, Inc.
    Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
  • Publication number: 20110098360
    Abstract: Disclosed is a pharmaceutical composition containing a compound useful for inhibiting neurotoxicity caused by beta amyloid. The pharmaceutical composition of the present disclosure contains 1,3,5,7-tetrakis(aminomethyl)adamantane, an analogous compound thereof or a salt thereof as an active ingredient. The inventors have studied methods for reducing the toxicity of beta amyloid oligomers based on the formation mechanism of dodecamers in consideration of the fact that especially the dodecamers from among the beta amyloid oligomers exhibit a significant activity as a toxin for synapses and neurons in cranial nerve diseases. The inventors have confirmed that the disclosed compound can induce structural epitope deformation of the dodecamer and thereby reduce toxicity of the beta amyloid oligomers.
    Type: Application
    Filed: March 9, 2009
    Publication date: April 28, 2011
    Applicant: NANODIAMOND, INC.
    Inventors: Min Yung Lee, So-Yeop Han, Jun Mo Chung, Pyung Lim Han, Jung Min Koh, Ha Yan Oak, Eun Kyung Hwang, In Sun Baek
  • Publication number: 20110065766
    Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 17, 2011
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20110065762
    Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.
    Type: Application
    Filed: September 13, 2010
    Publication date: March 17, 2011
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20110009439
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: February 23, 2010
    Publication date: January 13, 2011
    Applicant: AQUINOX PHARMACEUTICALS INC.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Patent number: 7858660
    Abstract: Compositions, kits and methods are provided for the treatment or prophylaxis of influenza.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: December 28, 2010
    Assignee: Adamas Pharmaceuticals, Inc.
    Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
  • Patent number: 7582658
    Abstract: A novel compound represented by the following formula (1) or a salt thereof: wherein symbol “A” represents a saturated heterocyclic group, a 5-membered heteroaromatic group having two heteroatoms in the ring, a group represented by the formula A1 (R2, R3, and R4 represent hydrogen atom, hydroxyl group, etc.), etc., B represents a group represented by the formula B1 (R11 represents hydrogen atom, hydroxyl group, etc.), etc., R1 represents an alkyl group, and symbol “n” represents an integer of 2 to 6, which has a parathyroid hormone depressing action and showing low toxicity, and a medicament containing the compound or salt thereof as an active ingredient.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: September 1, 2009
    Assignee: Asahi Kasei Pharma Corporation
    Inventors: Shiro Miyoshi, Toshinori Ishizuya
  • Patent number: 7342135
    Abstract: 3(4),7(8)-bis(aminomethyl)bicyclo[4.3.0]nonane and a process for its preparation, wherein bicyclo[4.3.0]nona-3,7-diene is reacted with synthesis gas in a homogeneous organic phase in the presence of transition metal compounds of Group VIII of the Periodic Table containing complex-bound organophosphorus compounds, and excess organophosphorus compound, at temperatures of 70 to 160° C. and pressures of 5 to 35 MPa, and the 3(4),7(8)-bisformylbicyclo[4.3.0]nonane thus obtained is reductively aminated.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: March 11, 2008
    Assignee: Celanese Chemicals Europe GmbH
    Inventors: Helmut Springer, Paolo Bavaj
  • Publication number: 20040182690
    Abstract: A method for recovering hexamethylene diamine (HMD) from a mixture comprising HMD, 6-aminocapronitrile (ACN) tetrahydroazepine (THA), and ADN comprising:
    Type: Application
    Filed: March 7, 2003
    Publication date: September 23, 2004
    Inventor: John J. Ostermaier
  • Patent number: 6262309
    Abstract: Disclosed is a process for producing norbornane dimethylene amines wherein norbornane dicarbonitriles are hydrogenated by using a Raney cobalt catalyst containing manganese etc. in the presence of water in an amount of 0.1 to 1.5 moles per mole of the norbornane dicarbonitriles.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: July 17, 2001
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Isao Fukada, Seiichi Ishii, Hiroharu Kageyama, Hiroki Mizutani
  • Patent number: 5354901
    Abstract: Perfluoro(cycloaliphatic methyleneoxyalkylene) compositions are provided. These compositions comprise perfluoro(cycloaliphatic methyleneoxyalkylene) carbonyl fluoride compounds having (a) a perfluorocycloaliphatic moiety which can have up to two perfluoroalkyl substituents and a perfluoroalkylene substituent, and (b) a perfluoromethyleneoxyalkylene carbonyl fluoride radical, the methylene group of the radical being bonded to a ring carbon atom or the perfluoroalkylene substituent of the moiety and the alkylene group of the perfluoromethyleneoxyalkylene carbonyl fluoride being a perfluoro(methyl)methylene group, a perfluoroisopropyleneoxy(methyl)methylene group, or a poly(perfluoroisopropyleneoxy)perfluoro(methyl)methylene group having up to about 10 perfluoroisopropyleneoxy units.
    Type: Grant
    Filed: February 1, 1993
    Date of Patent: October 11, 1994
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Richard M. Flynn, Patricia M. Savu
  • Patent number: 5232836
    Abstract: Vitamin D derivatives corresponding to the following formula I ##STR1## in which R.sub.1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D.sub.2 (C.sup.20 to C.sup.28) or D.sub.3 (C.sup.20 to C.sup.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: August 3, 1993
    Assignee: Ire-Medgenix S.A.
    Inventors: Roger Bouillon, Pierre J. De Clerco, Pierre Eliard, Maurits Vanderwalle
  • Patent number: 5232526
    Abstract: This invention is for new compounds, namely, diethanolammoniummethylcubane nitrates, a composition of diethanolammonium methylcubyl nitrates - hydroxylammonium nitrate (HAN) solutions and their method of use as aqueous liquid gun propellant ingredients.
    Type: Grant
    Filed: July 10, 1992
    Date of Patent: August 3, 1993
    Assignee: Thiokol Corporation
    Inventors: Rodney L. Willer, Alfred G. Stern
  • Patent number: 5145874
    Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.
    Type: Grant
    Filed: February 25, 1991
    Date of Patent: September 8, 1992
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, by Vera M. Wallach, legal representative
  • Patent number: 5084592
    Abstract: Azulenesquaric acid dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each have specified meanings are prepared from azulene derivatives of the formula ##STR2## where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each have specified meanings as intermediates, and used in an optical recording medium.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: January 28, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Schrott, Peter Neumann, Sibylle Brosius, Helmut Barzynski, Klaus D. Schomann, Harald Kuppelmaier
  • Patent number: 5051409
    Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 4716248
    Abstract: New compounds having the formula:X--(YQNH.sub.2).sub.p Iwherein p is 1 or 2 and the residues QNH.sub.2 are the same or different and each is a residue of formula: ##STR1## wherein n is an integer from 1 to 15; R.sub.1 is C.sub.1 -C.sub.8 alkyl; R.sub.2 is C.sub.1 -C.sub.4 alkyl; or R.sub.1 and R.sub.2 ; together with the carbon atom to which they are attached, from a C.sub.5 -C.sub.8 cycloalkylene residue; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl or C.sub.6 -C.sub.10 aryl; and Y is a divalent residue of formula: ##STR2## wherein R.sub.4 and R.sub.5 are H or C.sub.1 -C.sub.4 alkyl or, when p is 1, the group R.sub.4, together with the group X, can form a tetramethylene chain substituted by the group QNH.sub.2, X is NH.sub.2 or QNH.sub.2 or X may be combined with R.sub.4 as hereinbefore defined; and, when p is 2, X is a direct bond or a --CH.sub.
    Type: Grant
    Filed: October 12, 1984
    Date of Patent: December 29, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Frederick H. Howell, Josef Pfeifer
  • Patent number: 4551552
    Abstract: A low temperature and pressure process for preparing rimantadine in high yields from 1-adamantyl methyl ketoxime is provided. The process comprises contacting a solution of the ketoxime with hydrogen in the presence of a platinum on carbon catalyst at a low temperature and pressure, e.g., room temperature and a pressure of about 25-115 psia (170-790 KPa) are preferred.
    Type: Grant
    Filed: May 23, 1984
    Date of Patent: November 5, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: John J. Liu
  • Patent number: 4500469
    Abstract: The bis(methylamine) of norbornane compounds which have at least one of the amine hydrogens substituted with hydroxyalkyl, methylenephosphonic, alkylenesulfonic, carboxylic acid radicals and salts of any of the acid radicals are useful as chelating, sequestering agents. The phosphonate substituted compounds are also useful as threshold agents.
    Type: Grant
    Filed: February 27, 1984
    Date of Patent: February 19, 1985
    Assignee: The Dow Chemical Company
    Inventors: Jaime Simon, Druce K. Crump, David A. Wilson
  • Patent number: 4454157
    Abstract: The invention relates to a pharmaceutical composition comprising a tetracyclononane derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen atoms or alkyl radicals and A is CH.sub.2 CH.sub.2 or CH--R.sup.4 in which R.sup.4 is a hydrogen atom or an alkyl, cyclohexyl, phenylalkyl or optionally-substituted phenyl radical, or a salt thereof. The majority of compounds of the formula II are novel and they are included within the scope of the invention, as are processes for their manufacture. Typical of the compounds disclosed is 8-(1-amino-ethyl)tetracyclo[4,3,0,0.sup.2,4,0.sup.3,7 ]nonane.
    Type: Grant
    Filed: August 17, 1982
    Date of Patent: June 12, 1984
    Assignee: Imperial Chemical Industries PLC
    Inventor: Douglas L. Swallow
  • Patent number: 4357352
    Abstract: The invention relates to a pharmaceutical composition comprising a tetracyclononane derivative of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen atoms or alkyl radicals and A is CH.sub.2 CH.sub.2 or CH--R.sup.4 in which R.sup.4 is a hydrogen atom or an alkyl, cyclohexyl, phenylalkyl or optionally-substituted phenyl radical, or a salt thereof. The majority of compounds of the formula II are novel and they are included within the scope of the invention, as are processes for their manufacture. Typical of the compounds disclosed is 8-(1-amino-ethyl)tetracyclo-[4,3,0,0.sup.2,4,0.sup.3,7 ]nonane.
    Type: Grant
    Filed: December 4, 1978
    Date of Patent: November 2, 1982
    Assignee: Imperial Chemical Industries Limited
    Inventor: Douglas L. Swallow