Cyano Or Hydrazino Containing Patents (Class 554/54)
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Patent number: 7161016Abstract: Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.Type: GrantFiled: November 24, 1999Date of Patent: January 9, 2007Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Atmaram Khanolkar, Andreas Goutopoulos
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Patent number: 6800770Abstract: The invention compounds and methods for the treatment of motor disorders. In particular, the invention provides eicosanoid analogs which are effective in ameliorating motor disorders such as spasticity caused by multiple sclerosis (MS).Type: GrantFiled: January 17, 2003Date of Patent: October 5, 2004Assignee: Virginia Commonwealth UniversityInventors: Billy Martin, Raj K. Razdan, Anu Mahadevan, David Baker
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Publication number: 20040122089Abstract: Analogs of andandamide and arvanil have been found to act preferential at CB1 and AR1 receptors, and at receptors other than CB1 and AR1. The analogs provide analgesic effects in vivo, and are useful in pain management. In addition, the analogs may be used as anti-proliferative/anti-tumor agents, vasodilators, and in other applications. Several of the anandamide and arvanil analogs are more potent than anandamide and arvanil.Type: ApplicationFiled: February 13, 2003Publication date: June 24, 2004Inventors: Billy R. Martin, Raj K. Razdan, Vincenzo Di Marzo
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Patent number: 6121470Abstract: Glycine derivatives represented by the following formula (1) and cleanser compositions containing the same: ##STR1## wherein R is a linear or branched alkyl group having 11 to 13 carbon atoms, a linear or branched alkenyl group having 11 to 13 carbon atoms, or a linear or branched hydroxyalkyl group having 11 to 13 carbon atoms, and M.sub.1 and M.sub.2 are the same or different from each other and each independently is a hydrogen atom, an alkali metal atom, 1/2 (an alkaline earth metal atom), an ammonium group, a monoalkanolammonium group having 1 to 22 carbon atoms, a dialkanolammonium group having 2 to 22 carbon atoms in total, a trialkanolammonium group having 3 to 22 carbon atoms in total, or a protonated basic amino acid, are excellent in foaming, detergency, comfort in use and safety, are antipollutive and can be used for various purposes, for example, a cleanser composition for the hair and body or tableware.Type: GrantFiled: September 23, 1996Date of Patent: September 19, 2000Assignee: Kao CorporationInventors: Masakatsu Takahashi, Hiromoto Mizushima, Hiroe Tanahashi, Toshio Nozaki
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Patent number: 5990083Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: March 13, 1997Date of Patent: November 23, 1999Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5869712Abstract: .alpha.-Amino-substituted acetic acids or acid salts of formula ##STR1## where R represents a hydrogen atom or an alkyl or alkoxy group X represents a hydrogen atom, an alkali metal or alkaline-earth metal or an ammonium residue characterized in that they are totally free of haloacetic acid and alkali metal halide. They are capable of being obtained by reaction, under hot conditions, of glyoxal, or of a precursor of glyoxal, with a secondary amine or one of its salts of formula ##STR2## where R represents a hydrogen atom or an alkyl or alkoxy group, optionally followed by hydrolysis. They may be used as amphoteric surface-active agents for the manufacture of cosmetic compositions.Type: GrantFiled: June 19, 1995Date of Patent: February 9, 1999Assignee: Rhone-Poulenc ChimieInventor: Jean-Marc Ricca
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Patent number: 5830870Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: December 4, 1996Date of Patent: November 3, 1998Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5808118Abstract: A pigment additive for improved dispersibility and reduction of photodegradation.Type: GrantFiled: February 25, 1997Date of Patent: September 15, 1998Inventor: George Kimball Atkinson
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Patent number: 5627182Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.Type: GrantFiled: July 25, 1996Date of Patent: May 6, 1997Assignee: Ciba Geigy CorporationInventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
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Patent number: 5614649Abstract: Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: November 3, 1995Date of Patent: March 25, 1997Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Patent number: 5550262Abstract: Disclosed herein are inbibitors of the multicatalytic protease enzyme which are represented by the general formula: ##STR1## Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.Type: GrantFiled: November 14, 1994Date of Patent: August 27, 1996Assignee: Cephalon, Inc.Inventors: Mohamed Iqbal, James L. Diebold, Robert Siman, Sankar Chatterjee, James C. Kauer
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Process for trans-6[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
Patent number: 5489690Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.Type: GrantFiled: May 15, 1995Date of Patent: February 6, 1996Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Tung V. Le, Thomas N. Nanninga -
Patent number: 5468888Abstract: The present invention relates to new lupane dervivatives of the general formula: ##STR1## to their salts, to their preparation and to the pharmaceutical compositions which contain them.Type: GrantFiled: May 12, 1994Date of Patent: November 21, 1995Assignee: Rhone-Poulenc Rorer S.A.Inventors: Romaine Bouboutou, Norbert Dereu, Michel Evers, Jean-Christophe Gueguen, Claude James, Christele Poujade, Daniel Reisdorf, Yves Ribeill, Francoise Soler
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Patent number: 5342952Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.Type: GrantFiled: October 12, 1993Date of Patent: August 30, 1994Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Tung V. Le, Thomas N. Nanninga
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Patent number: 5180737Abstract: Compound of the formula (I):Q.sup.1 Q(CR.sup.2 .dbd.CR.sup.3).sub.a (CR.sup.4 .dbd.CF)(CR.sup.5 .dbd.CR.sup.6).sub.b C(.dbd.O)NHR.sup.1 (1)or a salt thereof, wherein Q.sup.1 is a phenyl ring or a fused bicyclic ring system containing 9 or 10 ring carbon atoms at least one ring being aromatic, or Q.sup.1 is a dihalovinyl group; Q is an alkyl chain containing 1 to 12 carbon atoms and optionally containing one or two oxygen atoms and/or an unsaturated group --CR.sup.7 .dbd.CR.sup.8 --, or --C.dbd.C--, wherein R.sup.7 and R.sup.8 are selected from hydrogen or halo; a is 0 or 1; b is 0 or 1; the sum of a and b is 0 or 1; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and are independently selected from hydrogen, halo and C.sub.1-4 alkyl; R.sup.1 is selected from hydrogen and C.sub.1-6 hydrocarbyl optionally substituted by dioxalanyl, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy are disclosed which have pesticidal activity.Type: GrantFiled: June 8, 1989Date of Patent: January 19, 1993Assignee: Roussel UclafInventor: Robert J. Blade
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Patent number: 5166378Abstract: Mono-acylated hydrazines are prepared in high yield by reaction of a hydrazine salt with an azole derivative of acyl halide in the presence of a strong base. Useful hydrazine salts include those of the formula RNHNH.sub.2 .multidot.HX, where R is alkyl, aryl, aralkyl, acyl, aroyl, heterocyclic or heteroaryl, and HX is a mineral or organic acid. Useful azole derivatives include those of the formula R'CO--A, where R' is alkyl, aryl, aralkyl, heterocyclic or heteroaryl and A is an azole radical such as pyrrole, imidazole, pyrazole, triazole, tetrazole, indole or benzimidazole.Type: GrantFiled: May 24, 1990Date of Patent: November 24, 1992Assignee: Eastman Kodak CompanyInventors: Chang K. Kim, Francesco Debellis, Michael E. Campbell