Hydrazine Containing Patents (Class 564/81)
-
Patent number: 8980442Abstract: There are provided an aromatic monoamine derivative having a fluorene structure-containing organic group and an aromatic hydrocarbon group-containing organic group, and an organic electroluminescent element containing an organic thin film layer composed of a single layer or plural layers while including at least a light emitting layer, the organic thin film layer being between a cathode and an anode, wherein at least one layer of the organic thin film layer, particularly a hole transport layer, contains the aromatic amine derivative alone or as a component of a mixture. An organic electroluminescent element which maintains high luminous efficiency even if exposed to a high temperature environment, and has a low driving voltage and a long emission lifetime, and an aromatic amine derivative capable of realizing the organic electroluminescent element are provided.Type: GrantFiled: March 18, 2010Date of Patent: March 17, 2015Assignee: Mitsui Chemicals, Inc.Inventors: Nobuhiro Yabunouchi, Tomoki Kato, Takahiro Fujiyama, Yoshiyuki Totani
-
Publication number: 20150025042Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 16, 2013Publication date: January 22, 2015Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
-
Publication number: 20140378461Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides.Type: ApplicationFiled: February 14, 2013Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anthony Cornelius O'Sullivan, Olivier Loiseleur, Daniel Stierli, Torsten Luksch, Thomas Pitterna
-
Patent number: 8642761Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.Type: GrantFiled: November 18, 2011Date of Patent: February 4, 2014Assignee: Wilex AGInventors: Hugo Ziegler, Peter Wikstroem
-
Patent number: 8609720Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: August 20, 2007Date of Patent: December 17, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
-
Publication number: 20130158063Abstract: Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders.Type: ApplicationFiled: August 24, 2011Publication date: June 20, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Milton Lang Brown, Yali Kong, Yong Liu, Robert Glazer, York Tomita
-
Patent number: 8344180Abstract: Disclosed are compound having NPY Y5 receptor antagonistic activity of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is optionally substituted lower alkyl, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted cycloalkylene, or —NR2—X— may be a group of the formula: wherein a group of the formula: is piperidinediyl, piperazinediyl, pyridindiyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl, U is a bond, lower alkylene or lower alkenylene, Y is —OCONR7—, —CONR7— or —CSNR7—, R7 is hydrogen or lower alkyl, Z is optionally substituted carbocyclyl, or optionally substituted heterocyclyl, W is —S(?O)n-, n is 2, provided that Z is not carbocyclyl substituted with non-halogeno lower alkoxy, and provided that 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [2-[(5-chloro-1H-indole-2-carbonyl)-amino]-5 -(N?,N?-dimethyl-hydrazinocarbonyl)-cyclohexyl]-amide and 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [Type: GrantFiled: August 28, 2007Date of Patent: January 1, 2013Assignee: Shionogi & Co., Ltd.Inventor: Naoki Kouyama
-
Publication number: 20120178805Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: ApplicationFiled: March 13, 2012Publication date: July 12, 2012Inventor: Yousef Al-Abed
-
Patent number: 8088772Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting ofType: GrantFiled: December 11, 2007Date of Patent: January 3, 2012Assignee: The Genetics Company, Inc.Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Frank Jaschinski, Guy Lemaillet, Cornelia Marty-Ernst, Elena Marzi, Leonardo Scapozza
-
Patent number: 8071809Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: November 12, 2010Date of Patent: December 6, 2011Assignee: Ambrx, Inc.Inventors: Feng Tian, Zhenwei Miao
-
Patent number: 8026395Abstract: The present invention relates to simple, safe, high-yield methods of synthesizing VNP40101M, 1,2-bis(methylsulfonyl)-2-(2-chloroethyl)-2-(methylaminocarbonyl)hydrazine, an anti-neoplasia agent. One particularly preferred method uses methyl chloroformamide in a one-pot reaction at elevated temperatures to provide VNP40101M in high yield.Type: GrantFiled: May 27, 2009Date of Patent: September 27, 2011Assignee: Nanotherapeutics, Inc.Inventors: Xu Lin, Ivan King
-
Patent number: 8017628Abstract: Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.Type: GrantFiled: July 14, 2008Date of Patent: September 13, 2011Assignee: Merck Serono S.A.Inventors: Stephen Arkinstall, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean-Pierre Gotteland, Marco Biamonte
-
Patent number: 7888533Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: October 26, 2007Date of Patent: February 15, 2011Assignee: Ambrx, Inc.Inventors: Feng Tian, Zhenwei Miao
-
Patent number: 7842838Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: August 21, 2009Date of Patent: November 30, 2010Assignee: Anadys Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Frank Ruebsam, Martin Tran, Peter Dragovich, Liansheng Li, Douglas Eric Murphy, David Kucera, Zhongxiang Sun, Chinh Viet Tran
-
Publication number: 20100256096Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: January 17, 2007Publication date: October 7, 2010Inventors: Dongcheng Dai, Tove C. Bolken, Dennis E. Hruby, Thomas R. Bailey
-
Publication number: 20100249135Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting ofType: ApplicationFiled: December 11, 2007Publication date: September 30, 2010Applicant: THE GENETICS COMPANY, INC.Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Jaschinskin Frank, Guy Lemaillet, Cornelia Marty-Ernest, Elena Marzi, Leonardo Scapozza
-
Publication number: 20100191475Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.Type: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
-
Publication number: 20100069378Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: July 25, 2007Publication date: March 18, 2010Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de las Ermitas Alcalde-Pais, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
-
Publication number: 20100004295Abstract: Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl or the like, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted lower alkylene or the like, Y is —OCONR7— or the like, R7 is hydrogen, lower alkyl or the like, Z is optionally substituted carbocyclyl or the like, W is optionally substituted alkylene or the like.Type: ApplicationFiled: August 28, 2007Publication date: January 7, 2010Inventor: Naoki Kouyama
-
Patent number: 7468458Abstract: Disclosed herein are accelerants for the formation of oxime-containing compounds from the reaction of a carbonyl-containing compound and a hydroxylamine-containing compound. The oxime-containing compound, the carbonyl-containing compound and the hydroxylamine-containing compound can each be a non-natural amino acid or a non-natural amino acid polypeptide. Also disclosed is the use of such accelerants to form oxime-containing compounds, the resulting oxime-containing compounds, and reaction mixtures containing such accelerants.Type: GrantFiled: October 19, 2007Date of Patent: December 23, 2008Assignee: Amerx, Inc.Inventors: Feng Tian, Zhenwei Miao
-
Publication number: 20080249102Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.Type: ApplicationFiled: February 9, 2006Publication date: October 9, 2008Inventors: Jenny Ekegren, Anders Hallberg, Hans Wallberg, Bertil Samuelsson, Mahalingam Kannan
-
Patent number: 7432286Abstract: The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation.Type: GrantFiled: September 28, 2000Date of Patent: October 7, 2008Assignee: Laboratories Serono SAInventors: Stephen Arkinstall, Serge Halazy, Dennis Church, Montserrat Camps, Thomas Rueckle, Jean-Pierre Gotteland, Marco Biamonte
-
Patent number: 6908947Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: October 25, 2001Date of Patent: June 21, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
-
Patent number: 6809119Abstract: The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, neuropathic pain, Parkinson's disease, diabetic retinopathy, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.Type: GrantFiled: November 26, 2002Date of Patent: October 26, 2004Assignee: Warner-Lambert Company LLCInventors: Lain-Yen Hu, Suzanne Ross Kesten, Huangshu Lei, Todd Robert Ryder, David Juergen Wustrow
-
Patent number: 6730704Abstract: The present invention relates to 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines useful as hypoglycemic agents, and to a process for synthesis thereof. The present invention also relates to the synthesis of 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines as new hypoglycemic agents which may be useful in the treatment of diabetes.Type: GrantFiled: March 29, 2002Date of Patent: May 4, 2004Assignee: Council of Scientific & Industrial ResearchInventors: Ramalingam Thallapalli, Venkata Durga Nageswar Yadavalli, Ramakrishna Sistla, Adari Bhaskar Rao, Prakash Vamanrao Diwan, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan
-
Patent number: 6727282Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 9, 2002Date of Patent: April 27, 2004Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 6693136Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.Type: GrantFiled: July 26, 2002Date of Patent: February 17, 2004Assignee: Abbott LaboratoriesInventors: Chih-Hung Lee, Meiqun Jiang, Richard A. Perner, Arthur Gomtsyan, Erol K. Bayburt, Guo Zhu Zheng
-
Publication number: 20030204034Abstract: Control agents that have an oxygen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers, particularly vinyl monomers.Type: ApplicationFiled: March 22, 2002Publication date: October 30, 2003Applicant: Symyx Technologies, Inc.Inventors: Dominique Charmot, Han-Ting Chang, Manikandan Jayaraman, Victor Nava-Salgado
-
Patent number: 6482909Abstract: Control agents that have a nitrogen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers. These control agents provide superior properties for control of the polymerization and/or the properties of the polymers obtained and/or the monomers that may be polymerized. In some embodiments, a bulky group is pendant off the activated thiocarbonyl portion of the control agents. Multifunctional control agents provide the opportunity for a variety of structurally unique polymers, including block copolymers, stars and hyper-branched polymers.Type: GrantFiled: September 25, 2001Date of Patent: November 19, 2002Assignee: Symyx Technologies, Inc.Inventors: Dominique Charmot, Han Ting Chang, Yunxiao Li
-
Publication number: 20020165275Abstract: The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins, and to pharmaceutical compositions comprising one or more of the said compounds. The invention further relates to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders.Type: ApplicationFiled: January 25, 2002Publication date: November 7, 2002Inventors: Yong-Qian Wu, Sergei Belyakov, Gregory S. Hamilton, David Limburg, Joseph P. Steiner, Mark Vaal, Ling Wei, Douglas Wilkinson
-
Patent number: 6459001Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.Type: GrantFiled: January 25, 2001Date of Patent: October 1, 2002Assignees: Aventis Pharma S.A., GenetechInventors: Serge Bernard, Denis Carniato, Jean-Francois Gourvest, Jean-Georges Teutsch, Jochen Knolle, Hans-Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Thomas R. Gadek, Robert S. McDowell, Robert M. Pitti
-
Publication number: 20020120149Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: September 7, 2001Publication date: August 29, 2002Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
-
Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
-
Publication number: 20020035264Abstract: There is provided a pharmaceutical composition suitable for topical administration to an eye which contains a selective COX-2 inhibitory drug or nanoparticles of a drug of low water solubility, in a concentration effective for treatment and/or prophylaxis of a disorder in the eye, and one or more ophthalmically acceptable excipients that reduce rate of removal from the eye such that the composition has an effective residence time of about 2 to about 24 hours. Also provided is a method of treating and/or preventing a disorder in an eye, the method comprising administering to the eye a composition of the invention.Type: ApplicationFiled: July 12, 2001Publication date: March 21, 2002Inventors: Tugrul T. Kararli, Rebanta Bandyopadhyay, Satish K. Singh, Leslie C. Hawley
-
Patent number: 6348499Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: November 24, 1999Date of Patent: February 19, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
-
Patent number: 6333349Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.Type: GrantFiled: June 29, 1999Date of Patent: December 25, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
-
Patent number: 6291464Abstract: This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity, etc., and represented by general formula [I]. wherein R1 is lower alkyl, etc., R2 is aryl, etc., A is or —SO2—, Q is —N═CH—, etc., X is lower alkylene, etc., and R3 and R4 are taken together to form lower alkylene, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and a pharmaceutical composition comprising the same.Type: GrantFiled: August 17, 1999Date of Patent: September 18, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ichiro Shima, Kazuhiko Ohne
-
Patent number: 6284795Abstract: The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.Type: GrantFiled: August 18, 1999Date of Patent: September 4, 2001Assignee: Warner-Lambert CompanyInventors: Helen Tsenwhei Lee, Randy Ranjee Ramharack, Bruce David Roth, Karen Elaine Sexton
-
Patent number: 6265446Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represType: GrantFiled: November 22, 1999Date of Patent: July 24, 2001Assignee: Hoffmann-La Roche Inc..Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
-
Patent number: 6235787Abstract: Hydrazine derivatives of the formula wherein Y is CO or SO2; R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y is SO2 and is lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y is CO; and R3 is hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula X-aryl, X-heteroarType: GrantFiled: June 16, 1998Date of Patent: May 22, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
-
Patent number: 6221907Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.Type: GrantFiled: February 2, 1999Date of Patent: April 24, 2001Assignee: Hoechst Marion RousselInventors: Serge Bernard, Denis Carniato, Jean-Francois Gourvest, Jean-Georges Teutsch, Jochen Knolle, Hans-Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Thomas R. Gadek, Robert S. McDowell, Robert M. Pitti
-
Patent number: 6172108Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptorType: GrantFiled: December 16, 1999Date of Patent: January 9, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
-
Patent number: 6153795Abstract: Water-insoluble polymer resins containing ethylenediamine subunits which are N-substituted with a functional group chosen from the group consisting of --H, --CS.sub.2, --CH.sub.2 PO.sub.3 H, and --CH.sub.3, or which are N-quarternized as --[N(CH.sub.3).sub.2.sup..sym..crclbar. OH]--, and polysalts of these. The use of such resins in separating nitrites, organic chlorine compounds, (heavy) metal ions including radioactive metal ions, counteranions of metal ions, and aliphatic and aromatic aldehydes from dilute aqueous solutions, especially at low concentrations. A method of synthesizing epoxy carbamate resins without violent reaction by inverse suspension condensation in cold liquid paraffin or toluene, preferably with dimethyl formamide or 1-methyl-2-pyrrolidone as co-solvents.Type: GrantFiled: August 7, 1997Date of Patent: November 28, 2000Assignee: AAG Industries, Inc.Inventor: Niyazi Bi.cedilla.ak
-
Patent number: 6114372Abstract: Compounds of formula (I) having MMP and TNF inhibitory activity.Type: GrantFiled: October 2, 1998Date of Patent: September 5, 2000Assignee: Darwin Discovery LimitedInventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson, John Fraser Keily
-
Patent number: 6011177Abstract: 4-Sulfonamidophenyl hydrazines are prepared by reaction between the hydrazine, optionally substituted, and the corresponding 4-substituted benzenesulfonamides, where the 4-substitution is an appropriate leaving group, in the presence of water and the absence of dimethyl sulfoxide as a solvent. The result is a product of unusually high purity.Type: GrantFiled: November 26, 1997Date of Patent: January 4, 2000Assignee: Aerojet-General CorporationInventors: Thomas G. Archibald, James C. Barnard
-
Patent number: 5989774Abstract: A silver halide photographic material is disclosed containing a new type of hydrazide compound represented by following general formula I, the different symbols of which are defined in the description. ##STR1## In a preferred embodiment Q is pyridinium, substituted with a propargyllic group or butynyl group.The photographic material is preferably a graphic arts recording material. High gradation and excellent hard dot quality are obtained.Type: GrantFiled: September 10, 1998Date of Patent: November 23, 1999Assignee: Agfa-Gevaert, N.V.Inventors: Johan Loccufier, Stefaan Lingier, Paul Callant, Sabine Emmers
-
Patent number: 5981138Abstract: A hydrazine compound represented by the following formula (I):Ar.sub.1 --NH--NH--G.sub.1 --R.sub.1 (I)wherein Ar.sub.1 represents an aromatic group; G.sub.1 represents a carbonyl group, a sulfonyl group, a sulfoxy group, a phosphoryl group, an oxalyl group or an iminomethylene group; R.sub.1 represents a hydrogen atom or a block group; and at least one of Ar.sub.1 and R.sub.1 has a group represented by the following formula (II): ##STR1## wherein * represents a bond for connecting directly or through a liking group to Ar.sub.1 or R.sub.1 ; Z represents a nonmetallic atom group capable of forming a 5- or 6-membered unsaturated heterocyclic ring having a conjugated positive charge; and X.sup.- represents --O.sup.-, --S.sup.- or --N.sup.- --R.sub.2, wherein R.sub.2 represents an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group. Also disclosed is a silver halide photographic light-sensitive material containing the hydrazine compound.Type: GrantFiled: September 4, 1997Date of Patent: November 9, 1999Assignee: Fuji Photo Film Co., Ltd.Inventors: Hiroyuki Suzuki, Kohzaburoh Yamada, Hiroshi Takeuchi, Toshihide Ezoe, Takashi Hoshimiya
-
Patent number: 5877217Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) using compounds of the following formula I ##STR1## wherein alk is a straight or branched chain alkylene group containing from 2 to 8 carbon atoms, and R is a lower alkyl group containing from 1 to 6 carbon atoms; and their biologically or pharmaceutically acceptable acid addition salts. Accordingly, a compositions are disclosed which comprises these N-acylaminoalkylhydrazinecarboximidamides, which are capable of inhibiting the formation of advanced glycosylation endproducts of target proteins. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: December 23, 1996Date of Patent: March 2, 1999Assignee: Alteon Inc.Inventors: Peter C. Ulrich, Dilip R. Wagle
-
Patent number: 5856353Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: June 7, 1995Date of Patent: January 5, 1999Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti
-
Patent number: 5814656Abstract: A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically effective amount of nitric oxide sufficient to protect the tissue from sepsis- or shock-induced injury.Type: GrantFiled: October 2, 1997Date of Patent: September 29, 1998Assignee: The United States Of America, as represented by the Department Of Health And Human ServicesInventors: Joseph E. Saavedra, Larry K. Keefer