The Aryl Ring Or Ring System Is Polycyclo Patents (Class 564/378)
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Publication number: 20140336380Abstract: The present invention provides a process for the preparation of agomelatine and its intermediate compounds. The invention also provides an intermediate compound of agomelatine represented by Formula (V).Type: ApplicationFiled: November 21, 2012Publication date: November 13, 2014Inventors: Anu Mittal, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad, Sudershan Kumar Arora
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20110306794Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine hydrochloride salt of formula (I) i.e. Cinacalcet hydrochloride and its intermediates of formulae (VII) and (VIII) wherein Z is chloride or another pharmaceutically acceptable anionic counterion.Type: ApplicationFiled: February 16, 2010Publication date: December 15, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Nicola Catozzi, Livius Cotarca, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
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Publication number: 20110281954Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.Type: ApplicationFiled: May 17, 2011Publication date: November 17, 2011Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
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Publication number: 20110110842Abstract: Systems and methods for the extraction of carbon nanotubes (CNTs) by continuous and/or batch processing are disclosed. Generally, a carbon nanotube material including carbon nanotubes (CNTs), carbon nanoparticles (CNPs), and carboxylated carbon (CC) is provided and agitated to produce a well-dispersed mixture. The well-dispersed mixture can be allowed to stand in a vessel having a lower end and an upper end. In some cases, the CNPs settle at the lower end. In some cases, at least some of the CNTs and CC are disposed at the upper end and can be removed in a dispersion, which can be pH adjusted and/or filtered to extract the CNTs from the CC.Type: ApplicationFiled: December 15, 2010Publication date: May 12, 2011Inventor: Robert C. Haddon
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Publication number: 20100316557Abstract: Systems and methods for the purification of carbon nanotubes (CNTs) by continuous liquid extraction are disclosed. Carbon nanotubes are introduced to a flow of liquid that enables the separation of CNTs from impurities due to differences in the dispersibility of the CNTs and the impurities within the liquid. Examples of such impurities may include amorphous carbon, graphitic nanoparticles, and metal containing nanoparticles. The continuous extraction process may be performed in one or more stages, where one or more of extraction parameters may be varied between the stages of the continuous extraction process in order to effect removal of selected impurities from the CNTs. The extraction parameters may include, but are not limited to, the extraction liquid, the flow rate of the extraction liquid, the agitation of the liquid, and the pH of the liquid, and may be varied, depending on the impurity to be removed from the CNTs.Type: ApplicationFiled: June 10, 2010Publication date: December 16, 2010Applicant: Carbon Solutions, Inc.Inventor: Robert C. Haddon
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Publication number: 20090247472Abstract: This invention relates to compounds with the formula (I) given below or one of their pharmaceutically acceptable salts, as a medicine; Formula (I) of pharmaceutical compositions comprising one or more compounds with Formula (I) as active constituent, use of compounds with Formula (I) for the preparation of compositions designed to prevent or treat at least one illness involving an abnormal cellular proliferation, pro-apoptotic compositions and/or anti-proliferative compositions comprising at least one compound with Formula (I)/and the use of compounds with formula (I) as pro-apoptotic and/or anti-proliferative agents.Type: ApplicationFiled: April 25, 2007Publication date: October 1, 2009Applicants: FLUOFARMA, UNIVERSITE BORDEAUX 1, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Gaelle Depierre, Jean Dessolin, Michel Laguerre, Claude Commandeur
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Publication number: 20090179551Abstract: The present invention relates to novel organic electroluminescent compounds having an indenofluorene or a difluorene skeletal, and a display employing the same as an electroluminescent material. The organic electroluminescent compounds according to the invention exhibit good electroluminescent efficiency and excellent life property, so that an OLED device having very good operative lifetime can be advantageously prepared.Type: ApplicationFiled: November 22, 2006Publication date: July 16, 2009Inventors: Hyuck-Joo Kwon, Young-Jun Cho, Seung-Soo Yoon, Bong-Ok Kim, Sung-Min Kim
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Publication number: 20090137837Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.Type: ApplicationFiled: June 19, 2008Publication date: May 28, 2009Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
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Publication number: 20070236137Abstract: The present invention relates to aromatic amine derivatives having a specific structure; and organic electroluminescent devices comprising a cathode, an anode and one or plural organic thin film layers including at least a light emitting layer which are sandwiched between the cathode and the anode wherein at least one of the organic thin film layers contains the above aromatic amine derivatives in the form of a single substance or a component of a mixture. There are provided the organic electroluminescent devices exhibiting a long life and a high efficiency of light emission which are capable of emitting a blue light having a high color purity, as well as the aromatic amine derivatives capable of realizing such organic electroluminescent devices.Type: ApplicationFiled: March 2, 2007Publication date: October 11, 2007Applicant: Idemitsu Kosan Co., Ltd.Inventor: Masakazu FUNAHASHI
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 6979566Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: GrantFiled: February 1, 2003Date of Patent: December 27, 2005Assignee: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Patent number: 6787570Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.Type: GrantFiled: December 16, 2002Date of Patent: September 7, 2004Assignee: Pfizer, Inc.Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
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Publication number: 20040143022Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.Type: ApplicationFiled: January 12, 2004Publication date: July 22, 2004Applicants: Mayo Foundation for Medical Education and Research, Virginia Tech Intellectual Properties, Inc.Inventors: Elliott Richelson, Paul R. Carlier
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Patent number: 6710089Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: March 23, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677375Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-bis-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6653508Abstract: Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.Type: GrantFiled: January 16, 2002Date of Patent: November 25, 2003Assignee: Gruenenthal GmbHInventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
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Publication number: 20030166708Abstract: Cyclic substituted aminomethyl compounds of general formula IA and IB, methods for production thereof, intermediates in said production methods, a medicament containing at least one of said cyclic substituted aminomethyl compounds, the use of said cyclic substituted aminomethyl compounds for the production of a medicament, pharmaceutical compositions containing said compounds, and methods for the treatment of pain, incontinence, pruritis, tinnitus aurium and/or diarrhea using said pharmaceutical compositions.Type: ApplicationFiled: January 10, 2003Publication date: September 4, 2003Inventors: Oswald Karl Zimmer, Babette-Yvonne Koegel, Wolfgang Werner Alfred Strassburger
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Patent number: 6613805Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 16, 2001Date of Patent: September 2, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 6583183Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-fused-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: June 24, 2003Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6521667Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: GrantFiled: August 11, 1998Date of Patent: February 18, 2003Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, PLC, SmithKline Beecham, Corp.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6476075Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-bis-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: November 5, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6448295Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020103191Abstract: Dibenzofluorene derivatives having a formula selected from the group consisting of 1Type: ApplicationFiled: January 14, 2002Publication date: August 1, 2002Applicant: Board of Regents, The University of Texas SystemInventors: Frederick F. Becker, Bimal K. Banik
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Publication number: 20020099220Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: ApplicationFiled: October 19, 2001Publication date: July 25, 2002Applicant: NPS Pharmaceuticals, Inc.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6342532Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.Type: GrantFiled: October 6, 1999Date of Patent: January 29, 2002Assignee: NPS Pharmaceuticals, Inc.Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
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Patent number: 6313175Abstract: Novel meta substituted arylalkylamine compounds are disclosed. These compounds can be administered as small molecule drugs to treat diseases or conditions associated with insufficient serotonin mediated nerve transmission (e.g., depression and obesity).Type: GrantFiled: August 13, 1999Date of Patent: November 6, 2001Assignee: Biostream, Inc.Inventors: David R. Elmaleh, Alan J. Fischman
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Patent number: 6310107Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: June 21, 1999Date of Patent: October 30, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 6204391Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: GrantFiled: September 21, 1998Date of Patent: March 20, 2001Assignee: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Patent number: 6057371Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.Type: GrantFiled: June 10, 1992Date of Patent: May 2, 2000Assignee: Virginia Commonwealth UniversityInventor: Richard A. Glennon
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Patent number: 5981599Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.Type: GrantFiled: April 30, 1997Date of Patent: November 9, 1999Assignee: NPS Pharmaceuticals, Inc.Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
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Patent number: 5756769Abstract: A method for producing a propargylamine compound represented by the general formula (I): ##STR1## which comprises reacting a propargyl compound represented by the general formula (II): ##STR2## with an aromatic aldehyde represented by the general formula (III):ArCHO (III)and ammonia to obtain an imine compound represented by the general formula (IV): ##STR3## and hydrolyzing the resultant imine compound. It is to provide a method for producing a propargylamine compound from a propargyl compound by a simple operation without using a special facility, using ammonia as a reaction reagent, without producing a dipropatygylamine compound and a tripropargylamine compound as by-products.Type: GrantFiled: May 30, 1997Date of Patent: May 26, 1998Assignee: Sumitomo Chemical Company, Ltd.Inventors: Shinzo Seko, Akihiko Nakamura, Motoo Hazama
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Patent number: 5672738Abstract: Process for the preparation of 3-(N-aryl-amino)-propyl-2'-sulfatoethyl-sulfonyl compoundsCompounds of the formula (1)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OSO.sub.3 M(1)are prepared by reacting a compound of the formula (2) ##STR1## with 2-mercaptoethanol to give a compound of the formula (3)Ar--NH--(CH.sub.2).sub.3 --S--(CH.sub.2).sub.2 --OH (3)at temperatures from 90.degree. to 270.degree. C. in the presence of a catalytic amount of a base, subsequently oxidizing the compound of the formula (3) to give a compound of the formula (4)Ar--NH--(CH.sub.2).sub.3 --SO.sub.2 --(CH.sub.2).sub.2 --OH(4),and finally esterifying the compound of the formula (4) with at least one molar equivalent of sulfuric acid, oleum or halosulfonic acid to give a compound of the formula (1).Compounds of the formula (1) are valuable starting compounds for the preparation of reactive dyestuffs.Type: GrantFiled: November 17, 1995Date of Patent: September 30, 1997Assignee: Hoechst AktiengesellschaftInventors: Christian Schumacher, Michael Meier, Werner Hubert Russ
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Patent number: 5648541Abstract: A process for preparing an R enantiomer of a compound of the formula (I): ##STR1## wherein Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF.sub.3, CF.sub.2 H, CFH.sub.2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH.sub.2 CF.sub.3, OH, CN, NO.sub.2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH--Me), C(O)N-lower alkyl.sub.2 (e.g., C(O)NMe.sub.2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH--C(O)-lower alkyl (e.g., NH--C(O)Me), where "lower alkyl" is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I).Type: GrantFiled: September 28, 1995Date of Patent: July 15, 1997Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. VanWagenen, Robert M. Barmore
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Patent number: 5616803Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.Type: GrantFiled: October 6, 1995Date of Patent: April 1, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
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Patent number: 5519062Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: May 23, 1994Date of Patent: May 21, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5508306Abstract: This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z.sup.1 and Z.sup.2 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, OH, F, Cl, Br, I, NO.sub.2, CN, SO.sub.2 NHR.sup.3, NR.sup.4.sub.2, CONR.sup.3.sub.2, COR.sup.5 ; where each R.sup.1 and R.sup.2 is independently H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH.sub.2, NR.sup.4, S, S.dbd.O, SO.sub.2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where R.sup.4 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or COR.sup.3 ; and where R.sup.5 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl, C.sub.1 -C.sub.6 straight or branched chain alkoxy or OH.Type: GrantFiled: September 9, 1993Date of Patent: April 16, 1996Assignee: Synaptic Pharmaceutical CorporationInventors: George Chiu, Charles Gluchowski
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Patent number: 5504253Abstract: A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.Type: GrantFiled: July 15, 1994Date of Patent: April 2, 1996Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. VanWagenen, Thomas E. D'Ambra
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Patent number: 5326784Abstract: New cycloalkylalkylamines which are sigma-receptor ligands of formule (I) ##STR1## in which: R.sub.1 is H or lower alkyl; X and Y are H, OH, lower alkyl, lower alkoxy, halogen or nitrile; V.sub.1 and V.sub.2 together form a double bond attached to an oxygen atom or to a hydroxyimino radical, or are linked as an ethylenedioxy chain; A represents a valency bond, an oxygen atom, a methylene or an ethylene group; m is equal to 0, 1 or 2; n has the value of an integer from 1 to 5. Psychotropic drug which is also useful in gastroenterology.Type: GrantFiled: July 29, 1993Date of Patent: July 5, 1994Assignee: Institut de Recherche JouveinalInventors: Jean-Louis Junien, Alain Calvet, Henri Jacobelli, Francois Roman
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Patent number: 5292893Abstract: A process is provided for catalytically reducing imines, oximes, hydrazones and related compounds. Moreover, there is provided a process for the catalytic asymmetric reduction of imines, oximes, hydrazones, and the like, using enantiomerically enriched catalysts, to provide chiral amine reaction products which are enriched in one enantiomer. Catalytic asymmetric reduction can also be carried out using an achiral precatalyst in combination with aThe U.S. Government has rights in this invention pursuant to NIH Grant Number GM 34917.Type: GrantFiled: November 14, 1991Date of Patent: March 8, 1994Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Christopher A. Willoughby
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Patent number: 5225595Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.Type: GrantFiled: November 4, 1992Date of Patent: July 6, 1993Assignee: BASF AktiengesellschaftInventors: Bernd Siegel, Claus Marschner, Manfred Patsch
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Patent number: 5220067Abstract: This invention provides a process for directly preparing hydrohalide salts of arylethylamines from (.alpha.-chloro-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst in an organic acid in substantial absence of moisture. The process is illustrated by conversion of 4-hydroxy (.alpha.-chloro-.alpha.Type: GrantFiled: March 30, 1992Date of Patent: June 15, 1993Assignee: Hoechst Celanese CorporationInventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
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Patent number: 5220066Abstract: This invention provides a process for directly preparing arylethylamines and their salts from (.alpha.-halo-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst. The process is illustrated by conversion of 4-hydroxy-(.alpha.-chloro-.alpha.Type: GrantFiled: March 30, 1992Date of Patent: June 15, 1993Assignee: Hoechst Celanese CorporationInventors: Ahmed Tafesh, B. Frank Wood, Joseph A. McDonough, Graham N. Mott
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Patent number: 5180746Abstract: An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.Type: GrantFiled: February 15, 1990Date of Patent: January 19, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
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Patent number: 5177112Abstract: Certain novel compounds having the structural formula ##STR1## wherein R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.Type: GrantFiled: September 10, 1991Date of Patent: January 5, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
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Patent number: 5175368Abstract: Arylalkylamines (as the hydrochloride salt), e.g. tyramine hydrochloride, are prepared by hydrogenating substituted or unsubstituted aryl-.alpha.-oximinoalkyl ketones, e.g. p-hydroxyisonitroacetophenone, in either in an aqueous reaction medium comprising hydrochloric acid, essentially without the presence of a lower alkyl alcohol in said reaction medium, or in an aqueous reaction medium comprising water, hydrochloric acid, and a lower alkyl alcohol, wherein the alcohol comprises less than about 90% by volume of the reaction medium. A substituent on the aryl portion of the aryl-.alpha.-oximinoalkyl ketone must be on a position which activates the aromatic ring.Type: GrantFiled: June 29, 1992Date of Patent: December 29, 1992Assignee: Hoechst Celanese CorporationInventors: Ahmed M. Tafesh, Joseph A. McDonough, Graham N. Mott
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Patent number: 5166438Abstract: A charge transporting material comprising a 1,3-pentadiene derivative having formula (I):A--CH.dbd.CH--CH.dbd.CH--CH.sub.2 --A (I)wherein A represents a 9-anthryl group which may have a substituent, a N-substituted carbazolyl group which may have a substituent, a N-substituted phenothiazinyl group which may have a substituent or ##STR1## in which Ar represents an arylene group which may have a substituent, R.sup.1 and R.sup.2 each represent an alkyl group which may have a substituent, an aralkyl group which may have a substituent, or an aryl group which may have a substituent; an electrophotographic photoconductor comprising an electroconductive support and a photoconductive layer formed thereon, which comprises as an effective component at least one of the 1,3-pentadiene derivatives of the above formula (I); and novel 1,3-pentadiene derivatives of the formula (I), provided that in the formula (I), R.sup.1 and R.sup.2 cannot be a methyl group at the same time, are disclosed.Type: GrantFiled: August 23, 1991Date of Patent: November 24, 1992Assignees: Ricoh Company, Ltd., Hodogaya Chemical Co., Ltd.Inventors: Mitsuru Hashimoto, Masaomi Sasaki, Tomoyuki Shimada, Nobuo Suzuki, Takayuki Sakai, Susumu Suzuka
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Patent number: 5011998Abstract: A novel synthesis of aromatic tertiary amines involves reacting an aromatic anil and an aromatic ether in a molar ratio of 1:1; adjusting the ratio to 2:1 produces novel enamines and by employing a two step process for enamine production, various unsymmetrically substituted enamines can be obtained which are readily hydrolyzed to corresponding deoxybenzoins which in turn are readily oxidized to benzils, the aromatic tertiary amines may be used to produce charge transport layers in xerography, while the benzils may be used to produce a variety of desired polymers.Type: GrantFiled: January 6, 1990Date of Patent: April 30, 1991Inventors: Allan S. Hay, Martino Paventi
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Patent number: 4996235Abstract: The present invention provides 3,4-diphenylbutanamines capable of selectively inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: November 25, 1987Date of Patent: February 26, 1991Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong
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Patent number: 4980354Abstract: The invention relates to tetrahydronaphthalene and indane derivatives with the general formula I: ##STR1## wherein R.sup.1 represents zero to four substituents, which may be the same or different and are selected from OH, halogen, NO.sub.2, CN, CF.sub.3, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and unsubstituted or C.sub.1 -C.sub.4 alkyl substituted amino;R.sup.2 represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkenyl and C.sub.1 -C.sub.4 alkynyl which may be substituted by halogen;R.sup.3 and R.sup.4 represent independently H, C.sub.1 -C.sub.4 alkyl or form together with the nitrogen atom a 5- or 6-membered ring;n has the value 0 or 1;ALK is an aliphatic hydrocarbon with 1-8 carbon atoms and their pharmaceutically acceptable salts.These new compounds are typical monoamine reuptake blockers with additional .alpha..sub.2 antagonist activity and show strong anti-depressant activity without being sedative.Type: GrantFiled: September 14, 1989Date of Patent: December 25, 1990Assignee: Akzo N.V.Inventors: James Cairns, Duncan R. Rae