The Aryl Ring Or Ring System Is Polycyclo Patents (Class 564/387)
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Patent number: 6515181Abstract: A process for the preparation of terbinafine which comprises the reaction of tert-butylacetylene with a compound of formula (II) characterized in that the reaction is carried out in the presence of copper (I) salts and of a base, in the absence of palladium.Type: GrantFiled: February 28, 2002Date of Patent: February 4, 2003Assignee: Dipharma S.p.A.Inventors: Graziano Castaldi, Giuseppe Barreca, Renzo Rossi
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Patent number: 6495496Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.Type: GrantFiled: December 22, 2000Date of Patent: December 17, 2002Assignee: Infineum International Ltd.Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist
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Patent number: 6448295Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Publication number: 20020123651Abstract: A process for the preparation of terbinafine which comprises the reaction of tert-butylacetylene with a compound of formula (II) 1Type: ApplicationFiled: February 28, 2002Publication date: September 5, 2002Inventors: Graziano Castaldi, Giuseppe Barreca, Renzo Rossi
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Publication number: 20020115576Abstract: Low molecular weight Mannich base condensates of hydroxy aromatic compounds, an aldehyde; and an amine, wherein the combined number of substituent carbon atoms does not exceed 80. Such compounds are useful as soot dispersants in lubricating oils when used alone, or in combination with high molecular weight dispersants.Type: ApplicationFiled: December 22, 2000Publication date: August 22, 2002Inventors: Antonio Gutierrez, Mark G. Stevens, Ricardo A. Bloch, Robert A. Kleist
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Patent number: 6252114Abstract: The invention provides a process for the preparation of 4-(p-methoxyphenyl)-2-aminobutane represented by structural formula (1) as shown herein below: [C11H17ON=4-(p-methoxy phenyl)-2-amino butane] said process comprising the steps of, (a) isolating a phenolic compound 4-hydroxyphenyl)-butan-2-ol from the leaves of Taxus wallichiana by known methods, (b) treating the phenolic compound in aqueous mineral acid to obtain a phenolic halide derivative, (c) converting the phenolic halide derivative into its methyl ether by treating it with a methating agent, (d) reacting the methyl ether halide with azide to obtain an azido derivative, and (e) hydrogenating the azido compound to obtain 4-(p-methoxyphenyl)-2-aminobutane.Type: GrantFiled: March 24, 2000Date of Patent: June 26, 2001Assignee: Council of Scientific and Industrial ResearchInventors: Sunil Kumar Chattopadhyay, Koneni Venkata Sashidhara, Vinayak Tripathi, Arun Kumar Tripathi, Veena Prajapati, Sushil Kumar
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Patent number: 6114394Abstract: The present invention relates to polyamine derivatives of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof which are useful as radioprotective agents. It relates also to the use of polyamines of the formula RHN-(CH.sub.2).sub.m -NH-(CH.sub.2).sub.n -NH-(CH.sub.2).sub.m -NHR wherein m is an integer from 2 to 4, n is an integer from 3 to 10 and R is C.sub.2 -C.sub.6 alkyl or --(CH.sub.2).sub.p -Ar wherein Ar is phenyl or naphthyl and p is an integer from 0 to 2; and the pharmaceutically acceptable addition salts thereof as radioprotective agents.Type: GrantFiled: October 14, 1997Date of Patent: September 5, 2000Assignee: Merrell Pharmaceuticals Inc.Inventors: Michael L. Edwards, Ronald D. Snyder
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Patent number: 6001884Abstract: The present invention features molecules which can modulate one or activities of an inorganic ion receptor. Preferably, the molecule can mimic or block the effect of extracellular Ca.sup.2+ on a calcium receptor. The preferred use of such molecules is to treat diseases or disorders by altering inorganic ion receptor activity, preferably calcium receptor activity.Type: GrantFiled: June 6, 1995Date of Patent: December 14, 1999Assignee: NPS Pharmaceuticals, Inc.Inventors: Edward F. Nemeth, Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. Delmar, Scott T. Moe
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Patent number: 5981599Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.Type: GrantFiled: April 30, 1997Date of Patent: November 9, 1999Assignee: NPS Pharmaceuticals, Inc.Inventors: Scott T. Moe, Bradford C. Van Wagenen, Eric G. DelMar, Richard Trovato, Manuel F. Balandrin
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Patent number: 5817875Abstract: Process for the manufacture of naphthylmethylamine derivatives and among them terbinafine as potential antimycotic agents.Type: GrantFiled: September 19, 1996Date of Patent: October 6, 1998Inventors: Khashayar Karimian, Regis C. H. S. Leung-Toung, Yiwei Li, Tim Fat Tam
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Patent number: 5808098Abstract: 1. An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sub.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.Type: GrantFiled: April 29, 1997Date of Patent: September 15, 1998Assignee: Nissan Chemical Industries Ltd.Inventors: Hiroshi Kashihara, Mikio Suzuki, Yoshio Ohara
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Patent number: 5739374Abstract: 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: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5686616Abstract: A novel process for preparing an optically active amine by asymmetric hydrogenation of an imine compound, such as an imine compound prepared by condensing benzylamine and acetophenone, in the presence of a catalytic amount of an iridium-optically active phosphine complex and benzylamine or a benzylamine derivative. The present invention provides an optically active amine of high optical purity.Type: GrantFiled: March 14, 1996Date of Patent: November 11, 1997Assignee: Takasago International CorporationInventors: Kazuhide Tani, Tsuneaki Yamagata, Yasutaka Kataoka, Hidenori Kumobayashi
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Patent number: 5633405Abstract: An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.Type: GrantFiled: May 25, 1995Date of Patent: May 27, 1997Assignee: Merck & Co., Inc.Inventors: Andrew S. Thompson, Edward G. Corley, Edward J.J. Grabowski, Nobuyoshi Yasuda
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Patent number: 5571942Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.Type: GrantFiled: August 22, 1995Date of Patent: November 5, 1996Assignee: Eli Lilly and CompanyInventors: Craig S. Hoechstetter, Diane L. Huser, John M. Schaus, Robert D. Titus
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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: 5436354Abstract: (E)-N-(3-Chloro-2-propenyl)-N-methyl-1naphthylenemethanamine and (E)-3-chloro-N-(3-chloro-2-propenyl)-N-methylbenzo[b]thiophene-7-methanami ne which are useful as intermediates in the production of enyne compounds which exhibit squalene epoxidase inhibiting activity and anti-Eumycetes activity.Type: GrantFiled: December 13, 1994Date of Patent: July 25, 1995Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Susumu Nakagawa, Akira Asai, Satoru Kuroyanagi, Makoto Ishihara, Yoshiharu Tanaka
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Patent number: 5430063Abstract: The invention concerns a phenoxyphenyl compound having the formula ##STR1## wherein R is one or two halogen atoms; andA is CH.sub.2 NR.sub.1 R.sub.2 or 4,5-dihydro-1H-imidazole, in which R.sub.1 and R.sub.2 are independently selected from hydrogen and lower alkyl; ora pharmaceutically acceptable salt thereof.The compounds have long half-lives and can be used against depression.Type: GrantFiled: February 3, 1993Date of Patent: July 4, 1995Assignee: Akzo N.V.Inventors: Gerardus S. F. Ruigt, Dirk Leysen, Johannes H. Wieringa
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Patent number: 5359091Abstract: A compound of the formula: ##STR1## wherein R.sup.11 is hydrogen, lower alkyl, haloloweralkyl, lower alkenyl, lower alkynyl or cycloalkyl; R.sup.21 is a group of the formula: ##STR2## wherein each of R.sup.3, R.sup.31, and R.sup.32 which may be the same or different, is hydrogen or lower alkyl, each of R.sup.4, R.sup.5, R.sup.41 and R.sup.51, which may be the same or different, is hydrogen, halogen, hydroxyl, lower alkyl or lower alkoxy, R.sup.42 is hydroxyl, halogen, R.sup.8 --O--, or R.sup.6 --X--Y-- wherein R.sup.6 is phenyl or thienyl which may have one or two substituents each of X and Y, which may be the same or different, is oxygen, sulfur, carbonyl, --CHR.sup.8 -- or --NR.sup.b, or X and Y together form a vinylene group or an ethynylene group, provided that when either one of X and Y is oxygen, sulfur or --NR.sup.b, the other is carbonyl or --CHR.sup.a, and R.sup.Type: GrantFiled: November 18, 1993Date of Patent: October 25, 1994Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Susumu Nakagawa, Akira Asai, Satoru Kuroyanagi, Makoto Ishihara, Yoshiharu Tanaka
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Patent number: 5334628Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.Type: GrantFiled: December 31, 1992Date of Patent: August 2, 1994Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5216178Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.Type: GrantFiled: August 15, 1991Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 5202486Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.Type: GrantFiled: July 31, 1990Date of Patent: April 13, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Joel C. Barrish, Steven H. Spergel
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Patent number: 5180746Abstract: An aralkylamine compound of the formula ##STR1## wherein R.sup.1 means a hydrogen atom or a lower alkyl group; R.sup.2 means an aromatic group which may be substituted; R.sup.3 means a hydrogen atom, a lower alkyl group or an aromatic group which may be substituted; n means an integer of 0 to 7; ring A means a five-through eight-membered cyclic group which may be substituted and may contain one or two hetero atom(s) of O and S atoms as the ring-constituents; and ring B means a benzene ring which may be substituted, or a salt thereof, which is useful as an cholinesterase inhibitor and a cerebral function ameliorating agent.Type: GrantFiled: February 15, 1990Date of Patent: January 19, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka, Yuji Ishihara
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Patent number: 5166438Abstract: A charge transporting material comprising a 1,3-pentadiene derivative having formula (I):A--CH.dbd.CH--CH.dbd.CH--CH.sub.2 --A (I)wherein A represents a 9-anthryl group which may have a substituent, a N-substituted carbazolyl group which may have a substituent, a N-substituted phenothiazinyl group which may have a substituent or ##STR1## in which Ar represents an arylene group which may have a substituent, R.sup.1 and R.sup.2 each represent an alkyl group which may have a substituent, an aralkyl group which may have a substituent, or an aryl group which may have a substituent; an electrophotographic photoconductor comprising an electroconductive support and a photoconductive layer formed thereon, which comprises as an effective component at least one of the 1,3-pentadiene derivatives of the above formula (I); and novel 1,3-pentadiene derivatives of the formula (I), provided that in the formula (I), R.sup.1 and R.sup.2 cannot be a methyl group at the same time, are disclosed.Type: GrantFiled: August 23, 1991Date of Patent: November 24, 1992Assignees: Ricoh Company, Ltd., Hodogaya Chemical Co., Ltd.Inventors: Mitsuru Hashimoto, Masaomi Sasaki, Tomoyuki Shimada, Nobuo Suzuki, Takayuki Sakai, Susumu Suzuka
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Patent number: 5149714Abstract: The present invention provides novel aryloxy indanamines of the formula ##STR1## wherein n, p and q are each independently 0, 1 or 2,Y and X are each independently lower alkyl, lower alkoxy, hydroxy, CF.sub.3, halogeno or when p or q are 2 and each of the Y or each of the X groups are on adjacent aryl carbon atoms, both of the X or both of the Y groups can be taken together to form a methylenedioxy moiety,R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, aralkyl, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached are pyrrolidino, morpholino, piperidino, piperazino, or 4-methylpiperazino,or an acid addition salt thereof, which are useful as antidepressants and as inhibitors of synaptic norepinephrine and serotonin uptake.Type: GrantFiled: August 15, 1990Date of Patent: September 22, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Jules Freedman
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Patent number: 5132459Abstract: Compounds of formula I ##STR1## wherein R.sub.Type: GrantFiled: July 21, 1989Date of Patent: July 21, 1992Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 5126371Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.Type: GrantFiled: August 20, 1990Date of Patent: June 30, 1992Assignee: BASF AkteingesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 5117062Abstract: A novel synthesis of aromatic tertiary amines involves reacting an aromatic anil and an aromatic ether in a molar ratio of 1:1; adjusting the ratio to 2:1 produces novel enamines and by employing a two step process for enamine production, various unsymmetrically substituted enamines can be obtained which are readily hydrolyzed to corresponding deoxybenzoins which in turn are readily oxidized to benzils, the aromatic tertiary amines may be used to produce charge transport layers in xerography, while the benzils may be used to produce a variety of desired polymers.Type: GrantFiled: January 22, 1991Date of Patent: May 26, 1992Inventors: Allan S. Hay, Martino Paventi
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Patent number: 5032616Abstract: 4-trans-substituted cyclohexylamine derivatives of the formula ##STR1## where R.sup.1 is the group CR.sup.5 R.sup.6 R.sup.7, in which R.sup.5, R.sup.6 and R.sup.7 are hydrogen, unsubstituted or substituted alkyl, alkoxy, alkylthio or cycloalkyl, with the proviso that not more than one of the substituents R.sup.5, R.sup.6 and R.sup.7 may by hydrogen, or in which R.sup.6 and R.sup.7 together with the included carbon atom form a three-membered to six-membered carbocyclic aliphatic ring,R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl or alkynyl or cycloalkyl or cycloalkenyl, which in turn may be substituted, with the proviso that the sum of the carbon atoms and hetero atoms (O, S and halogen) of R.sup.2 and R.sup.3 together is not less than 8,R.sup.4 is hydrogen, alkyl, cycloalkyl or alkoxy, and m is 1 to 4, and the bond is a single or a double bond,salts thereof, and their use as fungicides.Type: GrantFiled: August 28, 1987Date of Patent: July 16, 1991Inventors: Hubert Sauter, Matthias Zipplies, Norbert Goetz, Eberhard Ammermann, Ernst-Heinrich Pommer
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Patent number: 5030625Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 indpendently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2 CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u,in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.Type: GrantFiled: August 14, 1989Date of Patent: July 9, 1991Assignee: Sandoz Ltd.Inventor: Anton Stuetz
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Patent number: 5021458Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.Type: GrantFiled: December 7, 1988Date of Patent: June 4, 1991Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
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Patent number: 5019598Abstract: o-Aminomethylphenols of the formula ##STR1## where R.sup.1, R.sup.3 and R.sup.4 are hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy or dimethylamino, R.sup.2 is hydrogen, chlorine, bromine, alkyl, alkenyl, alkoxyalkyl, cyclohexyl or phenyl, or R.sup.1 and R.sub.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 form a carbocyclic, saturated or unsaturated five-membered or six-membered ring, and R is alkyl, and salts thereof, and fungicides containing these compounds.Type: GrantFiled: June 15, 1989Date of Patent: May 28, 1991Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Eberhard Ammermann, Gisela Lorenz
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Patent number: 4996235Abstract: The present invention provides 3,4-diphenylbutanamines capable of selectively inhibiting the uptake of serotonin and norepinephrine.Type: GrantFiled: November 25, 1987Date of Patent: February 26, 1991Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4957914Abstract: 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.Type: GrantFiled: August 12, 1988Date of Patent: September 18, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: Robin D. Clark, Jacob Berger, Klaus K. Weinhardt
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Patent number: 4946863Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: January 18, 1989Date of Patent: August 7, 1990Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4939148Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## and R.sub.2 represents hydrogen or lower alkyl, orR.sub.1 and R.sub.2 together with the carbon atom to which they are attached represent a group of formula IIg ##STR3## R.sub.4 and R.sub.5 represent independently hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl or halogenalkyl andR.sub.6 represents a group of formula ##STR4## R.sub.1 represents a group of formula IIa to IIf as defined above, R.sub.2 and R.sub.3 together form a --(CH.sub.2)--.sub.u group wherein u stands for a whole number from 1 to 8 and R.sub.4, R.sub.5 and R.sub.6 have the meanings given above.which compounds are indicated for use as pharmaceuticals and agrochemicals.Type: GrantFiled: January 29, 1987Date of Patent: July 3, 1990Assignee: Sandoz, Ltd.Inventors: Anton Stutz, Peter Nussbaumer
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Patent number: 4894392Abstract: Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance host resistance to infectious organisms. Such agents are administered prophylactically to individuals whose resistance to infection is comprised by chemotherapy, surgery, burns or other forms of severe stress.Type: GrantFiled: May 12, 1988Date of Patent: January 16, 1990Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, Timothy F. Gallagher
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Patent number: 4882358Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4 or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar being planar or deviating only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: May 12, 1987Date of Patent: November 21, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4847254Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: February 12, 1988Date of Patent: July 11, 1989Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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Patent number: 4837307Abstract: A 2,2'-bridged[1,1'-biphenyl]-3-ylmethyl compound of the following formula is an intermediate to insecticidal esters. ##STR1## wherein n is 1-4 and Y is a leaving group readily displaced by carboxylate anions.Type: GrantFiled: January 16, 1984Date of Patent: June 6, 1989Assignee: FMC CorporationInventor: Ernest L. Plummer
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Patent number: 4829090Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: May 9, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4827034Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 20, 1988Date of Patent: May 2, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4822822Abstract: Benzylamine derivatives having the general formula ##STR1## wherein R.sub.1 is an iso-propyl or tert-butyl group, R.sub.2 is a group of the formula: ##STR2## and R.sub.3 is a lower alkyl or lower alkenyl group, or its acid addition salt. These derivatives are useful for the treatment of animal epidemics or infectious diseases induced by fungi as an antimycotic agent for humans and animals, for the control of plant diseases as an agricultural fungicide, and for the control of fungi and bacteria in industrial materials or products as an industrial fungicide.Type: GrantFiled: October 27, 1986Date of Patent: April 18, 1989Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Masanobu Arita, Kiyoshi Arai, Nobuo Komoto, Setsuko Hirose, Takeshi Sekine
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Patent number: 4820873Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a pyrene or substituted pyrene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: September 28, 1987Date of Patent: April 11, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4818443Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: April 4, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4814502Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: March 21, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4810823Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: December 21, 1987Date of Patent: March 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair