Acyclic Nitrogen Bonded Directly To Chalcogen Patents (Class 546/338)
-
Patent number: 5728838Abstract: A process for the preparation of a compound of structural formula I ##STR1## wherein R.sup.1 is alkyl, alkenyl, phenyl or substituted phenyl, which comprises the addition of R.sup.1 to an intermediate 2: ##STR2## by treatment of 2 with (R.sup.1).sub.3 M followed by reductive removal of the sulfinyl group.Type: GrantFiled: April 2, 1997Date of Patent: March 17, 1998Assignee: Merck & Co., Inc.Inventors: Ioannis Houpis, Audrey Molina, Ralph P. Volante
-
Patent number: 5723475Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.Type: GrantFiled: October 28, 1996Date of Patent: March 3, 1998Assignee: Suntory LimitedInventors: Hirokazu Annoura, Mayumi Uesugi, Atsuko Fukunaga, Shigeki Tamura
-
Patent number: 5714615Abstract: Methods for using novel quaternary pyridinium compounds in inhibiting acetylcholinesterase in mammals, specifically using the quaternary pyridinium compounds in the prophylaxis and treatment of organophosphate poisoning and mammalian dementia by mimicking or opposing the actions of the natural neurotransmitter acetylcholine.Type: GrantFiled: February 8, 1994Date of Patent: February 3, 1998Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Jerry J. Buccafusco, Kenneth M. Starks
-
Patent number: 5629323Abstract: Amide Derivatives of formula (I) wherein R.sup.1 is a mono or bicyclic heteroaryl radical, R.sup.2 is cycloalkyl, R.sup.3 and R.sup.4 each represent hydrogen or lower alkyl, and R.sup.5 is a group of formula (A) or (B) or (C): R.sup.8 --CH.sub.2 --CH.sub.2 -- or (D) or (E): R.sup.9 OCH.sub.2 CHOHCH.sub.2 -- or (F): R.sup.9 OCH.sub.2 CH.sub.2 -- and their pharmaceutically acceptable salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics.Type: GrantFiled: May 25, 1995Date of Patent: May 13, 1997Assignee: John Wyeth & Brother, Ltd.Inventors: Ian A. Cliffe, Anderson D. Ifill
-
Patent number: 5612358Abstract: An insecticidal compound of the formula ##STR1## wherein A completes a 5 or 6 membered aromatic ring selected from the group pyridyl, pyridyl substituted with C.sub.1-5 alkyl, C.sub.1-5 haloalkyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, C.sub.1-5 alkylsulfonyl, cyano, halogen, phenoxy or C.sub.1-5 dialkylamino, pyrazinyl, pyrazinyl substituted with C.sub.1-5 alkyl or halogen, pyrazolyl substitited with C.sub.1-5 alkyl, pyridazyl substituted with halogen, or thiazolyl substituted with halogen or C.sub.1-5 alkyl;R.sub.1 is hydrogen or C.sub.1-5 alkyl, C.sub.1-5 haloalkyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, C.sub.1-5 alkylsulfonyl, cyano, halogen, phenoxy, or C.sub.1-5 dialkylamino;X is substituted or unsubstituted C.sub.1-3 alkylene or C.sub.1-3 alkylidene;R.sub.2 is hydrogen, monoalkylcarbamoyl, C.sub.1-5 dialkylcarbamoyl, C.sub.1-5 alkoyl, C.sub.1-5 alkyl substituted with halogen, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, C.sub.1-5 alkoxycarbonyl, cyano, aryl, haloaryl, C.sub.Type: GrantFiled: September 7, 1993Date of Patent: March 18, 1997Assignee: Nippon Soda Co., Ltd.Inventors: Keiichi Ishimitsu, Haruhito Ohishi, Renpei Hatano, Jun Mitsui, Junji Suzuki, Tomio Yamada, Nobuo Takakusa
-
Patent number: 5596008Abstract: A class of substitute pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1 is haloalkyl; wherein R.sup.2 is aryl optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfinyl, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, halo, alkoxy and alkylthio; wherein R.sup.3 is aryl substituted at a substitutable position with a radical selected from alkylsulfonyl and sulfamyl; and wherein R.sup.4 is selected from halo, alkoxy and alkynyloxy; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: February 10, 1995Date of Patent: January 21, 1997Assignee: G. D. Searle & Co.Inventor: Len F. Lee
-
Patent number: 5561142Abstract: Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: May 22, 1995Date of Patent: October 1, 1996Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, Elizabeth M. Naylor, Dong Ok, Ann E. Weber, Thomas Shih, Hyun Ok
-
Patent number: 5559150Abstract: The present invention is directed to novel compounds that are non-peptidic thrombin inhibitors. The compounds have the structure: ##STR1## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is one of alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; and n is from zero to five. The compounds of the invention are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventor: Richard M. Soll
-
Patent number: 5545741Abstract: The invention relates to a process for the preparation of racemic or optically active epibatidine of the Formula XIV ##STR1## which comprises subjecting racemic or optically active epi-epibatidine-of the Formula XIII ##STR2## to epimerization in the presence base. The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions too.Epibatidine is a known highly affective analgesic active ingredient.Type: GrantFiled: December 5, 1994Date of Patent: August 13, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Csaba Sz antay, Zsuzsanna B. Kardos, Istv an Moldvai, Eszter T. Major, Csaba Sz antay, Jr., Attila M andi, G abor Blask o, Gyula Simig, Gy orgyi Lax, S andor Drabant, Tamas Sz all asi, M arton Fekete, G abor Gigler
-
Patent number: 5532375Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.Type: GrantFiled: September 30, 1994Date of Patent: July 2, 1996Assignee: Roussel-UCLAFInventors: Giulio Galliani, Fernando Barzashi, Alina Butti, Carla Bonetti, Emilio Toja
-
Patent number: 5486528Abstract: Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.Type: GrantFiled: April 11, 1994Date of Patent: January 23, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Judit Bajnogel, Gabor Blasko, Zoltan Budai, Eva Schmidt, Andras Egyed, Marton Fekete, Istvan Gacsalyi, Istvan Gyertyan, Tibor Mezei, Kalara Reiter nee Esses, Gyula Simig, Katalin Szemeredi, Enik Szirt nee Kiszelly
-
Patent number: 5457131Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 18, 1994Date of Patent: October 10, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5457118Type: GrantFiled: April 20, 1994Date of Patent: October 10, 1995Assignee: Pfizer Inc.Inventors: Roger P. Dickinson, Kevin N. Dack, John Steele
-
Patent number: 5439910Abstract: Compounds having formula (I) ##STR1## wherein R.sup.1, R.sup.2 and A are defined as in the specification. The compounds are useful as fungicides.Type: GrantFiled: October 12, 1993Date of Patent: August 8, 1995Assignee: Zeneca LimitedInventors: Paul J. de Fraine, John M. Clough, Paul A. Worthington, Brian L. Pilkington, Ian R. Matthews
-
Patent number: 5420287Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, methyl, ethyl, fluoro, hydroxymethyl, carbomethoxy, trifluoromethyl, carboxyl and fluoromethyl; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.9, R.sup.11 and R.sup.12 is independently selected from hydrido, methyl, fluoro and chloro; and wherein each of R.sup.5 and R.sup.10 is independently selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, methoxy, methylthio, cyano, trifluoromethyl, hydroxymethyl, methoxymethyl, methylsulfonyl and sulfamyl; provided that when A is ##STR3## R.sup.5 cannot be hydrido when R.sup.10 is selected from hydrido, cyano, halo, methyl, trifluoromethyl and methoxy.; further provided that R.sup.10 cannot be hydrido when R.sup.Type: GrantFiled: June 3, 1994Date of Patent: May 30, 1995Assignee: G. D. Searle & Co.Inventors: David B. Reitz, Jinglin Li
-
Patent number: 5387608Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.Type: GrantFiled: August 17, 1993Date of Patent: February 7, 1995Assignee: Allergan, Inc.Inventor: Steven W. Andrews
-
Patent number: 5374641Abstract: Illustrative examples of the N-(3-pyridylalkyl)sulfonamide derivative are represented by the following formulae [II] and [III]: ##STR1## The derivatives are available for a thromboxane A.sub.2 production inhibitor, a thromboxane A.sub.2 antagonist, a prostaglandin H.sub.2 antagonist, an anti-thrombus agent, a thrombus-preventing agent and an anti-allergy agent.Type: GrantFiled: February 24, 1992Date of Patent: December 20, 1994Assignee: Terumo Kabushiki KaishaInventors: Hiroyuki Ohnishi, Masazumi Miyakoshi, Masashi Isozaki, Masayuki Fujitake, deceased, Naoya Mikami, Ryohei Yanoshita, Harue Akasofu, Katsuyoshi Sugizaki, Nobuyuki Nakata
-
Patent number: 5356914Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.Type: GrantFiled: April 5, 1993Date of Patent: October 18, 1994Assignee: Beecham Group p.l.c.Inventors: Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
-
Patent number: 5304566Abstract: The present invention relates to a compound having the formula below which has an excellent inseciticidal activity: ##STR1## wherein R.sub.1 represents an optionally substituted 5-6 membered aromatic hetero ring containing nitrogen atom, except a non-substituted 2-pyridyl; x represents an optionally substituted C.sub.1-3 alkyleneR.sub.2 represents a hydrogen, a carbamoyl, a mono or di C.sub.1-5 alkyl carbamoyl, a thiocarbamoyl, a mono or di C.sub.1-5 alkylthiocarbamoyl, a sulfamoyl, a mono or di C.sub.1-5 alkylsulfamoyl, an optionally substituted C.sub.1-5 alkyl, an optionally substituted C.sub.2-5 alkenyl, an optionally substituted C.sub.2-5 alkynyl, an optionally substituted C.sub.3-8 cycloalkyl, an optionally substituted C.sub.3-8 cycloalkenyl, an optionally substituted aryl or --Y--R.sub.5 ;Y represents O, S(O).sub.n, CO, CS or CO.sub.2 ;n represents 0, 1 or 2;R.sub.5 represents a hydrogen, an optionally substituted C.sub.1-5 alkyl, an optionally substituted C.sub.2-5 alkenyl, an optionally substituted C.Type: GrantFiled: July 9, 1991Date of Patent: April 19, 1994Assignee: Nippon Soda Co., LtdInventors: Keiichi Ishimitsu, Junji Suzuki, Haruhito Ohishi, Tomio Yamada, Renpei Hatano, Nobuo Takakusha, Jun Mitsui
-
Patent number: 5290756Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.Type: GrantFiled: June 8, 1982Date of Patent: March 1, 1994Assignee: Rohm and Haas CompanyInventors: Colin Swithenbank, Ted Fujimoto
-
Patent number: 5290942Abstract: Quaternary pyridinium compounds for use as acetylcholinesterase inhibitors of the following formulas: ##STR1##Type: GrantFiled: January 19, 1993Date of Patent: March 1, 1994Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
-
Patent number: 5284853Abstract: The invention provides novel 2, 3, 6 substituted quinazolinones of the formula ##STR1## wherein, R, R.sup.6 and X are defined in the specification which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: February 8, 1994Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan
-
Patent number: 5245034Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: March 23, 1992Date of Patent: September 14, 1993Assignee: Kiroyoshi HidakaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
-
Patent number: 5245040Abstract: A process for the preparation of 1,3-disubstituted 2-nitroguanidines of the formula I ##STR1## in which R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or a radical --CH.sub.2 B; A is an unsubstituted or mono- to tetrasubstituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical, which may contain one or two substituents from the group comprising C.sub.1 -C.sub.3 haloalkyl having 1 to 7 halogen atoms, cyclopropyl, halocyclopropyl having 1 to 3 halogen atoms, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl, C.sub.2 -C.sub.3 haloalkenyl and C.sub.2 -C.sub.3 haloalkynyl having 1 to 4 halogen atoms, C.sub.1 -C.sub.3 haloalkoxy having 1 to 7 halogen atoms, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkylthio having 1 to 7 halogen atoms, allyloxy, propargyloxy, allylthio, propargylthio, haloallyloxy, haloallylthio, cyano and nitro and one to four substituents from the group comprising C.sub.1 -C.sub.3 alkyl, C.sub.Type: GrantFiled: October 16, 1991Date of Patent: September 14, 1993Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Odd Kristiansen, Laurenz Gsell
-
Compounds of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime which are useful as cholinergic agents
Patent number: 5219872Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.Type: GrantFiled: February 26, 1987Date of Patent: June 15, 1993Assignee: Roussel UCLAFInventors: Giulio Galliani, Fernando Barzaghi, Alina Butti, Carla Bonetti, Emilio Toja -
Patent number: 5219873Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dimentia and memory disorders of the formula ##STR1## in which R represents hydrogen, hydroxyl, a linear, branched or cyclic, saturated or unsaturated, alkyl, containing up to 8 carbon atoms, possibly substituted by free or esterified carboxy or R represents aralkyl containing up to 10 carbon atoms or --COOZ in which Z represents a linear, branched or cyclic saturated or unsaturated, alkyl containing up to 8 carbon atoms and R.sub.2 represents hydrogen or a linear or branched, saturated or unsaturated alkyl containing up to 8 carbon atoms, COalk.sub.1 radical or (CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl containing up to 8 carbon atoms, as well as their addition salts with acids provided that if R represents an alkyl R.sub.2 does not represent hydrogen; also therapeutic compositions containing at least one said compound and method of treating patients with said compounds.Type: GrantFiled: September 15, 1989Date of Patent: June 15, 1993Assignee: Roussel UCLAFInventors: Giulio Galliani, Fernando Barzaghi, Carla Bonetti, Emilio Toja
-
Patent number: 5216150Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: September 12, 1991Date of Patent: June 1, 1993Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Hiroyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
-
Patent number: 5208343Abstract: Pharmaceutically useful compounds in the treatment of depression, psychoses, and inflammatory diseases having the following structure: ##STR1##Type: GrantFiled: March 24, 1992Date of Patent: May 4, 1993Assignee: Warner-Lambert CompanyInventors: Yazhong Pei, Haile Tecle
-
Patent number: 5206371Abstract: Quaternary pyridinium compounds, their use in inhibiting acetylcholinesterase, their roles in the prophylaxis and treatment of organophosphate poisoning, their roles in anticholinesterase therapy and their roles as agents mimicking or opposing the actions of the natural neurotransmitter acetylcholine.Type: GrantFiled: June 2, 1992Date of Patent: April 27, 1993Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
-
Patent number: 5187170Abstract: Thiocarboxylic esters of the formula I ##STR1## where the substituents have the following meanings: X is oxygen, sulfur, oxymethylene, methyleneoxy, thiomethylene, methylenethio, ethylene, ethenylene or ethynylene,Y,Z are each sulfur or oxygen, but Y and Z are not simultaneously oxygen,R is alkyl, mononuclear, dinuclear or trinuclear aryl or hetaryl, where aryl and hetaryl may be substituted,and fungicidal agents containing these compounds.Type: GrantFiled: February 4, 1992Date of Patent: February 16, 1993Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Siegbert Brand, Bernd Wenderoth, Gisela Lorenz, Eberhard Ammermann
-
Patent number: 5166416Abstract: The invention relates to new propenone oxime ethers, a method of preparing them and pharmaceutical compositions containing them.Said new propenone oxime ethers have the formula ##STR1## in which--Ar and Ar' each independentlyl denotes a phenyl group non-substituted, mono or polysubstituted, a 9-anthryl group or a naphthyl group, a pyridyl, thienyl or furyl group;R.sub.1 R.sub.2 each independently denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or together with the N-atom to which they are bonded a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl group;M=H, Cl, Br or a C.sub.1 -C.sub.6 alkyl groupn=2 or 3.The invention also deals with the salts of compounds of formula (I). Said compounds have good activity in the anti platelet-clotting tests and are also antagonists of the 5HT.sub.2 receptors.Type: GrantFiled: December 1, 1989Date of Patent: November 24, 1992Assignee: Societe Anonyme: SanofiInventors: Christian Congy, Patrick Gueule, Bernard Labeeuw, Murielle Rinaldi
-
Patent number: 5162329Abstract: .beta.-picoline derivatives of the formula ##STR1## where A is CR.sup.1 R.sup.2, R.sup.1 and R.sup.2 independently of each other are hydrogen, alkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together form a methylene chain,B is one of the groups CH.sub.2, CHOR.sup.3, CHalR.sup.4, C.dbd.O or C.dbd.N-O-R.sup.5, R.sup.3 being hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, acyl, phenyl, benzyl or benzoyl, where the phenyl ring is substituted or unsubstituted, R.sup.4 being hydrogen, fluorine, chlorine, bromine or iodine, R.sup.5 being hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, phenyl or benzyl, the phenyl ring being substituted or unsubstituted,Ar is a substituted or unsubstituted aryl radical,their N-oxides and plant-tolerated acid addition salts, and fungicides containing these compounds.Type: GrantFiled: May 23, 1991Date of Patent: November 10, 1992Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Bernhard Zipperer, Norbert Goetz, Michael Keil, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5162347Abstract: A piperidine compound has the generic formula and is useful to treat arrhythmia. ##STR1## in which R1 is a lower alkyl and W is: ##STR2## X is --S--, --SO-- or --SO2--, R2 is hydrogen or --(CH2)n--Y, n is an integer of 1 to 5, Y is an aryl, pyridyl or a substituted pyridyl, X' is --CO-- or --CH(OH)--,p is an integer of 1 to 4, R12 is hydrogen or a lower alkyl, Y' is --(CH2)m--A, m is 1 or 2, A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl, R12 and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents andR22 is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.Type: GrantFiled: May 20, 1991Date of Patent: November 10, 1992Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
-
Patent number: 5151428Abstract: A pyridine derivative of the formula: ##STR1## wherein R.sup.1 is, the same or different, each a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy gorup, a C.sub.1 -C.sub.3 haloalkoxy group, a cyano group or a nitro group; R.sup.2 is, the same or different, each a hydrogen atom, a halogen atom or a methyl group; R.sup.3 is a halogen atom or a C.sub.1 -C.sub.3 alkyl group; R.sub.4 is a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group; R.sup.5 is, the same or different, each a halogen atom, a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 haloalkyl group, a C.sub.1 -C.sub.3 alkoxy group or a C.sub.1 -C.sub.3 haloalkoxy group; X is an oxygen atom, a sulfur atom, a carbonyl group, a sulfinyl group, a sulfonyl group, an imino group or a methylene group; Y is an oxygen atom or a sulfur atom; l is an integer of 1 to 5; m is an integer of 1 to 3; and n is an integer of 1 to 4, which is useful for control of insect pest.Type: GrantFiled: May 24, 1991Date of Patent: September 29, 1992Inventors: Noriyasu Sakamoto, Hirosi Kisida, Hiroaki Fujimoto, Kimitoshi Umeda, Noritada Matsuo
-
Patent number: 5098924Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.Type: GrantFiled: September 15, 1989Date of Patent: March 24, 1992Assignee: E. R. Squibb & Sons, Inc.Inventor: Michael A. Poss
-
Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
-
Patent number: 5079361Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.Type: GrantFiled: September 9, 1988Date of Patent: January 7, 1992Assignee: Celltech LimitedInventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
-
Patent number: 5036073Abstract: Fungicidal substituted pyridine derivatives of the formula ##STR1## in which Ar stands for optionally substituted aryl,X stands for oxygen, sulphur, sulphinyl, sulphonyl or for one of the groups --CH.sub.2 --; --O--CH.sub.2 --; --CH.sub.2 --O--; --O--CH.sub.2 --CH.sub.2 --; --S(O).sub.n --CH.sub.2 --; --CH.sub.2 --S(O).sub.n -- or --S(O).sub.n --CH.sub.2 --CH.sub.2 --,in whichn in each case stands for the number 0, 1 or 2,R stands for alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl or for in each case optionally substituted aryl, aralkyl, aryloxyalkyl or arylthioalkyl andm stands for the number 0 or 1,and plant-compatible acid and metal salt addition products thereof. Intermediates of the formula ##STR2## are also new.Type: GrantFiled: November 28, 1989Date of Patent: July 30, 1991Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Wilhelm Brandes, Stefan Dutzmann, Gerd Hanssler
-
Patent number: 5028714Abstract: There are disclosed a pyrazole compound represented by the formula ##STR1## wherein the substituents of R.sub.1 to R.sub.7 and the symbol Z have the specified meanings as described in the text, an insecticidal, acaricidal and fungicidal composition containing the same, use of said composition for control of insects, acarids and fungi and a method of preparing said compound, and its intermediate.Type: GrantFiled: October 12, 1990Date of Patent: July 2, 1991Assignee: Sumitomo Chemical Company, LimitedInventors: Naoto Meki, Kazue Nishida, Tomotoshi Imahase, Hiroaki Fujimoto, Kenichi Mikitani, Hirotaka Takano, Yoriko Ogasawara, Masahiro Tamaki
-
Patent number: 5008276Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 17, 1988Date of Patent: April 16, 1991Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
-
Patent number: 4963682Abstract: A dihydropyridine.rarw..fwdarw. pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.rarw. .fwdarw. pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated.This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.Type: GrantFiled: August 21, 1987Date of Patent: October 16, 1990Assignee: University of FloridaInventor: Nicholas S. Bodor
-
Patent number: 4956003Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the disclosure, and the use thereof for combating unwanted plants, especially Gramineae.Type: GrantFiled: March 27, 1989Date of Patent: September 11, 1990Assignee: BASF AktiengesellschaftInventors: Dieter Jahn, Rainer Becker, Norbert Goetz, Bruno Wuerzer
-
Patent number: 4954523Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower aralalkyl, --CH2--NHSO3--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: June 9, 1989Date of Patent: September 4, 1990Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
-
Patent number: 4929734Abstract: Certain N-substituted 1-(1,2,3,6-tetrahydro-3-pyridinyl)oximes and N-substituted 1-(1,2,3,6-tetrahydro-4-pyridinyl)oximes are useful as sigma binding agents for the treatment of depression, psychoses and/or inflammatory diseases.Type: GrantFiled: October 18, 1988Date of Patent: May 29, 1990Assignee: Warner-Lambert CompanyInventors: Linda L. Coughenour, Robert E. Davis, David A. Downs, Thomas G. Heffner, Leonard T. Meltzer, Walter H. Moos, David W. Moreland, Haile Tecle
-
Patent number: 4920232Abstract: Known and novel substituted acroleins of the general formula I ##STR1## where R.sup.1 is alkoxy, phenoxy, halogen, haloalkyl, haloalkoxy, haloalkylthiyl or nitro, n is an integer from 1 to 5, in the case of n being greater than 1 the R.sup.1 s being identical or different and in the event of nitro substitution the aromatic ring carrying not more than 3 nitro groups, and where R.sup.2 is alkyl, cycloalkyl, unsubstituted or substituted aryl or hetaryl or a nonaromatic heterocyclic radical, are prepared by reacting a phenylacetaldehyde of the general formula II ##STR2## with an aldehyde of the general formula III[R.sup.2 -CHO] IIIin the presence of a base and a solvent. These acroleins are useful to prepare hydroxymethyloxiranes which are intermediates in the synthesis of antimycotic and fungicidal azoylmethyloxiranes.Type: GrantFiled: June 27, 1988Date of Patent: April 24, 1990Assignee: BASF AktiengesellschaftInventors: Norbert Goetz, Stefan Karbach, Hans-Gert Recker
-
Patent number: 4918067Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.Type: GrantFiled: July 22, 1987Date of Patent: April 17, 1990Assignee: Beecham Group p.l.c.Inventors: Brian C. Gasson, Michael J. Pearson
-
Patent number: 4902699Abstract: Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R represents hydrogen or a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 8 carbon atoms, or the radical ##STR2## in which R.sub.1 represents a linear or branched, alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, a linear or branched, saturated or unsaturated, alkoxy containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or the radical ##STR3## in which R.sub.2 represents a linear or branched alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, aryl containing up to 14 carbon atoms, possibly substituted, or aralkyl containing up to 18 carbon atoms, possibly substituted, and R' represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, as well as their addition salts with organic or mineral acids.Type: GrantFiled: August 22, 1988Date of Patent: February 20, 1990Assignee: Roussel UclafInventors: Emilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
-
Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
-
Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
-
Patent number: 4874775Abstract: A series of novel N-pyrinidyl- and pyrimidinyl sulfonamides are useful as fungicides and herbicides particularly for the protection of plants from phytopathogens.Type: GrantFiled: June 11, 1985Date of Patent: October 17, 1989Assignee: Eli Lilly and CompanyInventors: Eriks V. Krumkalns, David L. Smiley