Polycyclo Ring System Patents (Class 564/456)
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Patent number: 9000047Abstract: 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: GrantFiled: May 24, 2010Date of Patent: April 7, 2015Assignee: Farmalider, S.A.Inventors: Pilar Navarro Medrano, Elisabet Gregori Puigjane, Marisol Montolio Del Olmo, Ana Jimenez Redondo, Jordi Mestres Lopez
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Publication number: 20140296223Abstract: 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: ApplicationFiled: August 31, 2012Publication date: October 2, 2014Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
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Publication number: 20130303805Abstract: 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: ApplicationFiled: January 16, 2012Publication date: November 14, 2013Applicant: Mitsubishi Gas Chemical Company, Inc.Inventors: Hisayuki Kuwahara, Tomotaka Wada
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Publication number: 20130072553Abstract: 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: ApplicationFiled: December 25, 2009Publication date: March 21, 2013Inventor: Lifeng Xu
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Publication number: 20130065966Abstract: 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: ApplicationFiled: May 24, 2010Publication date: March 14, 2013Applicant: FARMALIDER, S.A.Inventors: Pilar Navarro Medrano, Elisabet Gregori Puigjane, Marisol Montolio Del Olmo, Ana Jimenez Redondo, Jordi Mestres Lopez
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Publication number: 20120310022Abstract: 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: ApplicationFiled: November 25, 2010Publication date: December 6, 2012Inventors: Chandrashekhar Khandekar, Suguna Gopal, James Smith
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Publication number: 20120052019Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: ApplicationFiled: August 22, 2011Publication date: March 1, 2012Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20120028957Abstract: 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: ApplicationFiled: August 1, 2010Publication date: February 2, 2012Inventors: William F. DeGrado, Jun Wang
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Patent number: 8053603Abstract: 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: GrantFiled: December 21, 2006Date of Patent: November 8, 2011Assignee: 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
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Patent number: 7981930Abstract: 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: GrantFiled: February 29, 2008Date of Patent: July 19, 2011Assignee: Adamas Pharmaceuticals, Inc.Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
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Publication number: 20110098360Abstract: 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: ApplicationFiled: March 9, 2009Publication date: April 28, 2011Applicant: 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
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Publication number: 20110065762Abstract: 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: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20110065766Abstract: 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: ApplicationFiled: September 13, 2010Publication date: March 17, 2011Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
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Publication number: 20110009439Abstract: 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: ApplicationFiled: February 23, 2010Publication date: January 13, 2011Applicant: AQUINOX PHARMACEUTICALS INC.Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
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Patent number: 7858660Abstract: Compositions, kits and methods are provided for the treatment or prophylaxis of influenza.Type: GrantFiled: June 2, 2009Date of Patent: December 28, 2010Assignee: Adamas Pharmaceuticals, Inc.Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
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Patent number: 7582658Abstract: 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: GrantFiled: December 23, 2004Date of Patent: September 1, 2009Assignee: Asahi Kasei Pharma CorporationInventors: Shiro Miyoshi, Toshinori Ishizuya
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Patent number: 7342135Abstract: 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: GrantFiled: January 25, 2007Date of Patent: March 11, 2008Assignee: Celanese Chemicals Europe GmbHInventors: Helmut Springer, Paolo Bavaj
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Publication number: 20040182690Abstract: A method for recovering hexamethylene diamine (HMD) from a mixture comprising HMD, 6-aminocapronitrile (ACN) tetrahydroazepine (THA), and ADN comprising:Type: ApplicationFiled: March 7, 2003Publication date: September 23, 2004Inventor: John J. Ostermaier
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Patent number: 6262309Abstract: 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: GrantFiled: September 22, 2000Date of Patent: July 17, 2001Assignee: Mitsui Chemicals, Inc.Inventors: Isao Fukada, Seiichi Ishii, Hiroharu Kageyama, Hiroki Mizutani
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Patent number: 5354901Abstract: 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: GrantFiled: February 1, 1993Date of Patent: October 11, 1994Assignee: Minnesota Mining and Manufacturing CompanyInventors: Richard M. Flynn, Patricia M. Savu
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Patent number: 5232836Abstract: 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: GrantFiled: February 18, 1992Date of Patent: August 3, 1993Assignee: Ire-Medgenix S.A.Inventors: Roger Bouillon, Pierre J. De Clerco, Pierre Eliard, Maurits Vanderwalle
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Patent number: 5232526Abstract: 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: GrantFiled: July 10, 1992Date of Patent: August 3, 1993Assignee: Thiokol CorporationInventors: Rodney L. Willer, Alfred G. Stern
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Patent number: 5145874Abstract: 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: GrantFiled: February 25, 1991Date of Patent: September 8, 1992Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, by Vera M. Wallach, legal representative
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Patent number: 5084592Abstract: 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: GrantFiled: September 30, 1988Date of Patent: January 28, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Schrott, Peter Neumann, Sibylle Brosius, Helmut Barzynski, Klaus D. Schomann, Harald Kuppelmaier
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Patent number: 5051409Abstract: 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: GrantFiled: November 1, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 4716248Abstract: 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: GrantFiled: October 12, 1984Date of Patent: December 29, 1987Assignee: Ciba-Geigy CorporationInventors: Frederick H. Howell, Josef Pfeifer
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Patent number: 4551552Abstract: 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: GrantFiled: May 23, 1984Date of Patent: November 5, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: John J. Liu
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Patent number: 4500469Abstract: 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: GrantFiled: February 27, 1984Date of Patent: February 19, 1985Assignee: The Dow Chemical CompanyInventors: Jaime Simon, Druce K. Crump, David A. Wilson
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Patent number: 4454157Abstract: 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: GrantFiled: August 17, 1982Date of Patent: June 12, 1984Assignee: Imperial Chemical Industries PLCInventor: Douglas L. Swallow
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Patent number: 4357352Abstract: 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: GrantFiled: December 4, 1978Date of Patent: November 2, 1982Assignee: Imperial Chemical Industries LimitedInventor: Douglas L. Swallow
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Patent number: RE49811Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: GrantFiled: March 7, 2022Date of Patent: January 23, 2024Assignee: Apogee Biotechnology CorporationInventors: Charles D. Smith, Kevin J. French, Yan Zhuang