The Nitrogen Is Attached Indirectly To A Benzene Ring By Acyclic Nonionic Bonding Patents (Class 558/422)
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Publication number: 20020019374Abstract: Salicylohydrazide derivatives of the formula I 1Type: ApplicationFiled: June 14, 2001Publication date: February 14, 2002Inventors: Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 6346518Abstract: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.Type: GrantFiled: January 26, 1995Date of Patent: February 12, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Jean Louis Mesens, Jozef Peeters
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Patent number: 6344505Abstract: Provided is a composition which contains a mono- or bis-benzotriazole compound, an N-oxide thereof, or a mixture of at least two of the preceding compounds. Representative bis-benzotriazole compounds include 3,3′-bis-(2H-benzotriazol-2-yl)-5,5′-di-tert-octyl-1,1′-biphenyl-2,2′-diols. Representative mono-benzotriazole compounds include 3-(2H-benzotriazol-2-yl)-5,5′-di-tert-octyl-1,1′-biphenyl-2,2′-diols. These mono- and bis-benzotriazole compounds are useful as stabilizers of degradable polymers against the degradative action of ultraviolet light. Also provided is a method of making these benzotriazole compounds by oxidative dimerization of the corresponding monomeric benzotriazole or by reductive cyclization of the corresponding azo- compound.Type: GrantFiled: November 11, 1999Date of Patent: February 5, 2002Assignee: Cytec Industries Inc.Inventors: Donald H. Valentine, Jr., John F. Stephen, Thomas P. Sassi
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Patent number: 6284913Abstract: There is provided lower alkanesulphonate salts of cyanobenzylamines, which salts may be produced via a selective recrystallisation process. The salts may be produced advantageously following the selective hydrogenation of a dicyanobenzene to a cyanobenzylamine in the presence of a C3-5 alkyl alcohol.Type: GrantFiled: July 22, 1999Date of Patent: September 4, 2001Assignee: AstraZeneca ABInventors: Patric Fransson, Magnus Sjögren
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Patent number: 6265439Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases.Type: GrantFiled: April 3, 2000Date of Patent: July 24, 2001Assignee: G.D. Searle & Co.Inventors: Richard A Mueller, Thomas E Barta, John P McKearn, Susan A Gregory, Richard A Partis, Francis J Koszyk
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Patent number: 6251925Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,Type: GrantFiled: December 13, 2000Date of Patent: June 26, 2001Assignee: Glaxo Wellcome Inc.Inventors: Kelly Horne Donaldson, Barry George Shearer, David Edward Uehling
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Patent number: 6239288Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: March 2, 1999Date of Patent: May 29, 2001Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6229047Abstract: A nonlinear optical material which is characterized as having a relatively high macroscopic dipole moment achieved through the generally parallel packing of dipolar molecules in a relative orientation to reinforce their dipole moments. The nonlinear optical material may be a crystalline azine or imine bridged di-arene in which the arenyl groups, which can be the same or different, are substituted with an electron donor group on the first arenyl group Ar1 and A is an electron acceptor group which is substituted on the second arenyl group Ar2. B is an azine or imine bridge which extends between and interconnects the first and second arenyl groups. The nonlinear optical material has a dipole alignment factor of at least 0.1, more preferably, at least 0.5.Type: GrantFiled: December 4, 1995Date of Patent: May 8, 2001Assignee: The Curators of the University of MissouriInventors: Ranier E. Glaser, Grace S. Chen
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Patent number: 6114277Abstract: The object of the invention is to provide a process for preparing a cyano group-containing methylamine, comprising hydrogenating only one of the two nitrile groups of a aromatic dinitrile, wherein the aromatic dinitrile is reacted a a high conversion ratio using a small amount of a catalyst under the conditions of a low temperature and a low pressure to prepare a cyano group-containing aromatic methylamine in a high yield.Type: GrantFiled: September 30, 1998Date of Patent: September 5, 2000Assignee: Showa Denko K.K.Inventors: Motoo Miura, Yuseki Suyama, Hideyuki Kondo, Kouhei Morikawa
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Patent number: 6075049Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.Type: GrantFiled: April 23, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Rohl, Norbert Gotz, Michael Rack, Ruth Muller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6037472Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.Type: GrantFiled: November 22, 1994Date of Patent: March 14, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5948932Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: x is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ;Y is O, NRR.sup.1,R independently of one another are hydrogen and C.sub.1 -C.sub.4 -alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl and alkoxy;m is 0, 1 or 2, it being possible for the radicals R.sup.2 to be different when m is 2;R.sup.3 is hydrogen, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl;R.sup.4, R.sup.5 and R.sup.6 have the meanings given in claim 1,and their salts, a process and intermediates for the preparation of these compounds, and compositions comprising them for controlling animal pests and harmful fungi.Type: GrantFiled: April 15, 1998Date of Patent: September 7, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Herbert Bayer, Ruth Muller, Hubert Sauter, Reinhard Kirstgen, Volker Harries, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann
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Patent number: 5905090Abstract: Analogues of the active metabolite of leflunomide, and to the use thereof as immunosuppressive and/or antinflammatory agents.Type: GrantFiled: April 29, 1998Date of Patent: May 18, 1999Assignee: Italfarmaco S.p.A.Inventors: Giorgio Bertolini, Mauro Biffi, Flavio Leoni, Maria Letizia Marchetti, Jacques Mizrahi, Flavio Somenzi, Paolo Mascagni
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Patent number: 5847147Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0, 1, 2 or 3;Z is CN, CO-A or CS-A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R.sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.Type: GrantFiled: March 13, 1998Date of Patent: December 8, 1998Assignee: Novartis Corp.Inventors: Walter Kunz, Beat Jau
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Patent number: 5840764Abstract: The compound of the formula: ##STR1## wherein R.sup.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, or polyfluoroalkyl; and one of R.sup.2, R.sup.3 and R.sup.4 is hydroxyl and the other two are, independently, H, CN, halogen, alkyl or hydroxyl; or a pharmaceutically acceptable salt thereof, is useful as a smooth muscle relaxant.Type: GrantFiled: January 14, 1998Date of Patent: November 24, 1998Assignee: American Home Products CorporationInventors: Dominick A. Quagliato, Edward M. Matelan, Madelene M. Antane
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Patent number: 5821386Abstract: Disclosed are novel compounds which are dopamine reuptake blockers for treating cocaine abuse. The compounds are represented by the following structural formula: ##STR1## R2 is n-propyl, iso-propyl, n-butyl, sec-butyl, or tert-butyl. Phenyl Ring B is unsubstituted or substituted with one, two or three substituents.Type: GrantFiled: August 15, 1997Date of Patent: October 13, 1998Assignee: Allelix-Pharm-Eco L.P.Inventors: Mark Froimowitz, Kuo-Ming Wu
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Patent number: 5817877Abstract: A process of preparing an organic amine having at least one unsaturated group, such as an arylamine, involving contacting an unsaturated organic sulfonate, such as an aryl sulfonate, with a reactant amine, such as an alkyl or aryl amine, in the presence of a base and a transition metal catalyst under reaction conditions. The transition metal catalyst contains a Group 8 metal and a chelating ligand, for example a Group 15-substituted arylene or Group 15-substituted metallocene, such as 1,1'-bis(diphenylphosphino)-2,2'-binaphthyl or 1,1'-bis(diphenylphosphino)-ferrocene, respectively. The aryl sulfonate can be prepared from a phenol and sulfonating agent.Type: GrantFiled: September 19, 1997Date of Patent: October 6, 1998Assignee: Yale UniversityInventors: John F. Hartwig, Michael S. Driver, Janis Louie, Blake Hamann
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Patent number: 5817834Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.Type: GrantFiled: February 9, 1998Date of Patent: October 6, 1998Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5808080Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: May 2, 1997Date of Patent: September 15, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, David Andrew Neel, Mark Alan Winter
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Patent number: 5770758Abstract: Compounds of the formula I ##STR1## and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III ##STR2## In the compounds of the formulae I and III: X is halogen,n is 0,1,2 or 3;Z is CN, CO-A or CS-A,A is hydrogen, halogen, OR.sub.1, SR.sub.2 and N(R.sub.3)R.sub.4 ;R.sub.1 to R .sub.4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R.sub.3 and R.sub.Type: GrantFiled: December 20, 1996Date of Patent: June 23, 1998Assignee: Novartis CorporationInventors: Walter Kunz, Beat Jau
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Patent number: 5736568Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.Type: GrantFiled: November 25, 1996Date of Patent: April 7, 1998Assignee: Knoll AktiengesellschaftInventors: Paul Rafferty, Gerald Bernard Tometzki
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Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5693860Abstract: There are provided substituted acid amide, arylhydrazone compounds (amaidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: April 28, 1995Date of Patent: December 2, 1997Assignee: American Cyanamid CompanyInventors: Joseph Augustus Furch, David George Kuhn, David Allen Hunt
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Patent number: 5684200Abstract: Hydroxylamine ethers I ##STR1## (where X is NO.sub.2, CN, halogen, alkyl or haloalkyl, Y is H, NO.sub.2, CN, halogen, alkyl or haloalkyl, n is 0-2 or 1-4 where Y and all radicals X are halogen and Alk is unsubstituted or substituted alkylene) and their salts with mineral acids or strong organic acids are prepared by reacting either a hydroximino compound II ##STR2## (where R.sup.1 is alkyl, R.sup.2 is alkyl or alkoxy or R.sup.1 +R.sup.2 form an alkylene chain) in the presence of an alkali metal hydroxide, alkali metal alcoholate, alkali metal bicarbonate or alkali metal carbonate as the base, or the corresponding anion II directly, with an alkylating agent III ##STR3## (where R.sup.3 is unsubstituted or substituted alkyl or unsubstituted or substituted phenyl) to give an oximino derivative IV ##STR4## said derivative is cleaved by means of a mineral acid or a strong organic acid to give the salt of I and, if desired, the latter is converted by means of a base into the free compound I.Type: GrantFiled: June 6, 1995Date of Patent: November 4, 1997Assignee: BASF AktiengesellschaftInventors: Albrecht Harreus, Norbert Goetz, Volker Maywald, Harald Rang, Ulf Misslitz, Ulrich Klein
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Patent number: 5648386Abstract: The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.Type: GrantFiled: November 29, 1994Date of Patent: July 15, 1997Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Wolfgang Resemann, Adolf Durr, Gunther Engelhardt, John Frances Quirke
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Patent number: 5614630Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew G. Knapp, Lee D. Margolin
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Patent number: 5610191Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alky1,Y is a group ##STR2## R is hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl,and pesticides containing these compounds.Type: GrantFiled: November 22, 1995Date of Patent: March 11, 1997Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5527945Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: August 31, 1994Date of Patent: June 18, 1996Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5510529Abstract: Thioamides of the formula I ##STR1## where A, B, R' are hydrogen, cyano, alkyl, alkoxy or halogen,X is .dbd.CHCH.sub.3 or .dbd.N--OCH.sub.3,R.sup.1, R.sup.2 are hydrogen or alkyl,Y is a group --O--, --S--, ##STR2## --O--CH.sub.2, --CH.sub.2 --O--, --S--CH.sub.2 --, --CH.sub.2 --S--, --CH.sub.2 --CH.sub.2, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 --O--N.dbd.C(R')-- andR is hydrogen, unsubstituted or substituted alkyl, unsubstituted substituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted hetaryl, and pesticides containing these compounds.Type: GrantFiled: November 4, 1994Date of Patent: April 23, 1996Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Gisela Lorenz, Eberhard Ammermann
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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: 5436373Abstract: N-benzyl-N-organo-substituted aminoalkanol is prepared by reacting benzyl chloride or substituted benzyl chloride with an organo-substituted aminoalkanol in the presence of a molar excess of the starting aminoalkanol and, optionally, water, and in the absence of a) an organic solvent for the reactants and b) alkali metal hydroxide. A portion of the excess aminoalkanol may be substituted with an alternative amine or dissolved alkali metal carbonate.Type: GrantFiled: October 26, 1994Date of Patent: July 25, 1995Assignee: Elf Atochem North America, Inc.Inventors: Stanley R. Sandler, Doris L. Baer
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Patent number: 5428065Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 27, 1995Assignee: Lilly Industries LimitedInventors: Barry P. Clark, Graham H. Timms
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Patent number: 5411936Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,x is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: January 19, 1993Date of Patent: May 2, 1995Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5395957Abstract: The invention relates to the separation of enantiomers of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.Type: GrantFiled: December 14, 1993Date of Patent: March 7, 1995Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Wolfgang Resemann, Adolf Durr, Gunther Engelhardt, John F. Quirke
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Patent number: 5362747Abstract: 2-Nitroaryl or 2-cyanoaryl compounds of the formula ##STR1## pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.Type: GrantFiled: November 3, 1993Date of Patent: November 8, 1994Assignee: Abbott LaboratoriesInventors: Marlon Cowart, James F. Kerwin
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Patent number: 5310756Abstract: Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C.sub.1-6 -alkoxy, C.sub.1- -alkyl, C.sub.1-5 -alkanoyl, C.sub.3-5 -alkylene, aryloxy- or aralkoxy, andR is 3,4-methylenedioxy, aryl or heteroaryl which are optionally substituted with one or more cyano, halogeno, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkenyl, trifluoromethyl, C.sub.3-5 -alkylene, aryloxy or aralkoxy; andR.sup.1 and R.sup.2 independently is C.sub.1-10 -alkyl, C.sub.3-7 -cycloalkyl, C.sub.2-10 -alkenyl, C.sub.3-6 -cycloalkyl-C.sub.1-5 -alkyl, optionally substituted with C.sub.1-5 -alkoxy or cyano; orR.sup.1 and R.sup.2 may together form a carbocyclic ring and a salt thereof with a pharmaceutically acceptable acid,provided however that R.sup.1 is not C.sub.3-7 -cycloalkyl, C.sub.1-10 -alkyl, or alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C.sub.1-4 -alkoxy, aryloxy or cycloalkyl or cycloalkylalkyl, when X is H and R.sup.2 is a methyl group.Type: GrantFiled: June 12, 1992Date of Patent: May 10, 1994Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5308869Abstract: N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal, for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.Type: GrantFiled: March 30, 1992Date of Patent: May 3, 1994Assignee: State of Oregon, acting by and through the Oregon State Board of Higher EducationInventors: John F. W. Keana, Eckard Weber
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Patent number: 5306821Abstract: This invention relates to a novel process for the preparation of tertiary carbinamines by double addition of organolanthanide reagents, especially organocerium reagents, to nitriles. It further relates to the preparation of such amines by the addition of organolanthanide reagents to imines.Type: GrantFiled: January 10, 1992Date of Patent: April 26, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Engelbert Ciganek
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Patent number: 5290806Abstract: 4-4(tert-butylphenyl)-cyclohexylamines and quaternary ammonium salts thereof of the formulae ##STR1## where R.sup.1 is hydrogen, alkyl or alkenyl,R.sup.2 is alkyl, haloalkyl, hydroxyalkyl, cycloalkyl, alkylcycloalkyl, bicycloalkyl, alkenyl, unsubstituted or mon- to trisubstituted phenyl, or unsubstituted or mono- to trisubstituted phenylalkyl,X.crclbar. is a plant-tolerated acid anion,and their plant-tolerated acid addition salts, and fungicides containing these compounds.Type: GrantFiled: July 2, 1993Date of Patent: March 1, 1994Assignee: BASF AktiengesellschaftInventors: Bernhard Zipperer, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5272144Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.Type: GrantFiled: June 13, 1991Date of Patent: December 21, 1993Assignee: Farmitalia Carlo Erba s.r.l.Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
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Patent number: 5254595Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.Type: GrantFiled: January 9, 1992Date of Patent: October 19, 1993Assignee: Elf SanofiInventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
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Patent number: 5248695Abstract: The invention relates to the separation of enantiomers, of cimaterol, (-)-cimaterol, the addition salts thereof and processes for preparing them and their use in pharmaceutical compositions and animal feeds.Type: GrantFiled: April 30, 1991Date of Patent: September 28, 1993Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Wolfgang Resemann, Adolf Durr, Gunther Engelhardt, John F. Quirke
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Patent number: 5239084Abstract: Antimycotically-active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-7 -alkyl or C.sub.2-7 -alkenyl or together are a straight chain C.sub.2-4 -alkylene; R.sup.3 and R.sup.4 each independently are hydrogen or C.sub.1-7 -alkyl; R.sup.5 and R.sup.6 each independently are hydrogen, halogen, trifluoromethyl, nitro, cyano, C.sub.1-7 -alkoxy or C.sub.1-7 -alkyl; and Q is an unsubstituted or substituted phenyl or naphthyl group, wherein the substituents are at least one of halogen, trifluoromethyl, cyano, nitro, C.sub.1-7 -alkyl, C.sub.1-7 -alkoxy; C.sub.2-10 -alkenyl; or a substituted or unsubstituted C.sub.1-10 -alkyl group wherein said substituents are at least one hydroxy group; andpharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: September 10, 1992Date of Patent: August 24, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Guerry, Synese Jolidon
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Patent number: 5214046Abstract: The compound of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 individually is hydrogen, lower alkyl or lower alkenyl or together signify straight-chain alkylene with 2 to 4 carbon atoms, R.sup.3 is hydrogen, halogen or lower alkyl, Q is alkylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and each of Y and Y' individually is a direct bond or the group --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--, the group R.sup.1 R.sup.Type: GrantFiled: February 6, 1992Date of Patent: May 25, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Guerry, Synese Jolidon, Rene Zurfluh
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Patent number: 5200561Abstract: Disclosed is a process for producing an optically active amine represented by the formula (IV) ##STR1## wherein R.sub.7 and R.sub.8 each denote an alkyl group, aryl group or aralkyl group, providing that they do not denote the same group at the same time, and * indicates an asymmetric carbon atom, which comprises reacting an asymmetric reducing agent obtained from (1) an optically active amine derivative represented by the formula (I) ##STR2## wherein R.sub.1 denotes an alkyl group, aryl group or aralkyl group; R.sub.2 denotes a hydrogen atom, alkyl group or aralkyl group; R.sub.3 denotes an aryl group or a substituent represented by the formula (II) ##STR3## wherein R.sub.4 and R.sub.5 each denote a hydrogen atom, aryl group or aralkyl group, and * is as defined above, (2) a metal borohydride and (3) sulfuric acid, with either the syn-isomer or the anti-isomer of an oxime derivative represented by the formula (III) or with a mixture rich in either one of the two isomers ##STR4## wherein R.sub.Type: GrantFiled: October 7, 1991Date of Patent: April 6, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Naoto Konya, Yukio Yoneyoshi, Yoji Sakito, Shinji Nishii, Gohfu Suzukamo, Hiroko Sakane
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Patent number: 5198584Abstract: p-phenylenediamines having a quaternary ammonium group and substituted with an electron withdrawing group, derivatives thereof, compositions containing same, and their use as developers for dyeing keratinous fibers, are disclosed.Type: GrantFiled: June 4, 1992Date of Patent: March 30, 1993Assignee: Clairol Inc.Inventors: A. C. Chan, Y. G. Pan, D. L. Chang
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Patent number: 5185375Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Ar represents optionally substituted phenyl group, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl or two R.sup.1 substituents on the same nitrogen atom may together form optionally substituted alkylene, and salts thereof, processes for their preparation and compositions containing them are described.Type: GrantFiled: March 30, 1990Date of Patent: February 9, 1993Assignee: May & Baker LimitedInventors: David C. Cook, Terance W. Hart, Iain M. McLay, Malcolm N. Palfreyman, Roger J. A. Walsh
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Patent number: 5183940Abstract: Gallium is efficiently extracted from strongly basic solutions containing aluminates by extractants having the tris- and/or tetrakis (2-hydroxybenzyl)-1,2-diaminoethane chemical moiety. The diaminoethane derivative may be used together with a hydrocarbyl 8-hydroxyquinoline and/or with a tertiary carboxylic acid.Type: GrantFiled: May 11, 1991Date of Patent: February 2, 1993Assignee: Imperial Chemical Industries PLCInventors: Peter M. Quan, Stephen W. Leeming
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Patent number: RE34712Abstract: The two enantiomers of the anti-depressant drug of the formula I ##STR1## are disclosed. Methods for resolving intermediates and their .[.steroselective.]. .Iadd.stereoselective .Iaddend.conversion to a corresponding .[.enatiomer.]. .Iadd.enantiomer .Iaddend.of I are also disclosed.Type: GrantFiled: September 14, 1993Date of Patent: August 30, 1994Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard