Chalcogen Bonded Directly To The Carbon Patents (Class 544/397)
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Patent number: 11365195Abstract: Disclosed herein are a series of modafinil analogue compounds that bind with moderate to high affinity to the dopamine (DA) transporter (DAT) and several analogues also having affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. Employing aminopiperidine, piperidineamino, spirobicyclodiaza, or substituted piperazine functional groups, desired dopamine transporter affinity has been retained along with improved metabolic stability over unsubstituted piperazine ring analogues. Importantly, these compounds have no predicted addictive liability. Also disclosed are methods for treating substance use disorders as well as other neuropsychiatric disorders such as ADHD, depression, narcolepsy, and cognitive impairment.Type: GrantFiled: November 12, 2018Date of Patent: June 21, 2022Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Amy Hauck Newman, JoLynn Barbara Giancola, Rachel D. Slack
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Patent number: 8394954Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.Type: GrantFiled: March 26, 2008Date of Patent: March 12, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Bandari Rajendra Prasad
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Publication number: 20120277250Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: July 11, 2012Publication date: November 1, 2012Applicant: THERAVANCE, INC.Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
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Publication number: 20100174074Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.Type: ApplicationFiled: March 26, 2008Publication date: July 8, 2010Inventors: Ahmed Kamal, Bandari Rajendra Prasad
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Patent number: 7524846Abstract: The present invention is directed to arylalkyl- and cycloalkylalkyl-piperazine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: April 28, 2009Assignee: WyethInventor: Paige Erin Mahaney
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Patent number: 7491723Abstract: The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: February 17, 2009Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, William Jay Moore, Joseph Peter Sabatucci
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Patent number: 7419980Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Publication number: 20040097730Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein R2 is R3 is selected from the group consisting of 1) hydrogen, 2) halogen, 3) C 1-4 alkyl, 4) C 3-7 cycloalkyl, 5) CF3, 6) OCF3, 7) C 1-4 alkoxy, and 8) cyano; and R12 is a 5-membered heteroaryl ring having 2, 3, or 4 heteroatoms, provided that at least 1 heteroatom is N, and at most 1 of the heteroatoms is S, said ring being unsubstituted or substituted, at any one ring atom, with CH3.Type: ApplicationFiled: August 1, 2003Publication date: May 20, 2004Inventors: Mary Beth Young, Philippe G. Nantermet, Harold G. Selnick, Peter D. Williams
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Patent number: 6706745Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.Type: GrantFiled: May 18, 2000Date of Patent: March 16, 2004Assignee: Teijin LimitedInventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
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Patent number: 6214848Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.Type: GrantFiled: April 30, 1999Date of Patent: April 10, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
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Patent number: 6130222Abstract: Compounds of the formula (I) ##STR1## as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.Type: GrantFiled: April 24, 1997Date of Patent: October 10, 2000Assignee: Astra Pharma Inc.Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
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Patent number: 5962507Abstract: Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl having up to 17 carbon atoms.Type: GrantFiled: December 5, 1997Date of Patent: October 5, 1999Assignee: Dr. Karl Thomae GmbHInventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
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Patent number: 5919777Abstract: The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.Type: GrantFiled: April 23, 1997Date of Patent: July 6, 1999Assignee: Novo Nordisk A/SInventors: Thomas Kruse Hansen, Bernd Pesche, Knud Erik Andersen
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Patent number: 5840896Abstract: There is disclosed a process for preparing (l)-(-)-2-aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-?5,5-bis(4-fluor ophenyl)pentyl!-1-piperazineacetamide which comprises the steps of (a) cyclizing (-)-(S,S)-N.sup.1,N.sup.Type: GrantFiled: April 18, 1995Date of Patent: November 24, 1998Assignee: Janssen Pharmaceutica, N.V.Inventors: Herman Van Belle, Willy Joannes Carolus Van Laerhoven
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Patent number: 5432179Abstract: A piperazine derivative represented by the following formula: ##STR1## or a pharmaceutically acceptable salt thereof. The compound according to the present invention has strong anti-histaminic and anti-allergic affects and a high degree of safety, and is useful as an anti-histaminic agent, an anti-allergic agent and/or an anti-asthmatic drug. Also disclosed are pharmaceutical compositions containing the compound of formula 1 and a method for the treatment of allergic diseases comprising administering the claimed compound.Type: GrantFiled: December 30, 1993Date of Patent: July 11, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Kazuhiro Kumagai, Masaaki Nagasawa, Hidenori Takahashi, Tooru Abe, Takeshi Omata, Yoshihide Segawa
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Patent number: 5324728Abstract: A naphthoic acid derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, a lower alkanoyloxy group, a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or an aralkyloxy group;R.sub.4 is a hydrogen atom or a lower alkyl group;R.sub.5 is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaromatic group;X is a group ##STR2## a cycloalkylene group, a bivalent nitrogen-containing heterocyclic group, or a group ##STR3## --R.sub.8 --NH-- or --NH--R.sub.8, where R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group and R.sub.8 is a cycloalkylene group, or R.sub.6 and R.sub.7, together with R.sub.4, may form an alkylene group of 1-3 carbon atoms;Y is --S(O).sub.p --, --(CH.sub.2).sub.Type: GrantFiled: December 2, 1991Date of Patent: June 28, 1994Assignee: Fujirebio Inc.Inventors: Yasuo Sekine, Tetsuaki Yamaura, Masato Nishimura, Eri Kojima, Yasuko Emoto, Yasushi Higashide
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Patent number: 5308840Abstract: Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R.sup.8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.Type: GrantFiled: April 6, 1992Date of Patent: May 3, 1994Assignee: Green Cross CorporationInventors: Naoki Sugiyama, Fumihiko Akaboshi, Haruko Yakumaru, Tomokazu Gotoh, Masanori Sugiura, Shigeki Kuwahara, Masahiko Kajii, Yoshiko Tanaka, Takao Kondoh, Chikara Fukaya
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Patent number: 5276035Abstract: A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: May 4, 1992Date of Patent: January 4, 1994Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Erling Guddal, Erik B. Nielsen
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Patent number: 5066680Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.Type: GrantFiled: February 5, 1990Date of Patent: November 19, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5036098Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.Type: GrantFiled: September 14, 1989Date of Patent: July 30, 1991Assignee: Nippon Shinyaku Co., Ltd.Inventors: Kiyoshi Kimura, Masahiro Kise, Iwao Morita
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Patent number: 5028610Abstract: Compounds of formula (I):A--M--B-- (I)(in which: M represents a saturated heterocyclic group having from 5 to 7 ring atoms of which 2 are nitrogen atoms, said group being unsubstituted or being substituted at any of its carbon atoms by C.sub.1 -C.sub.6 alkyl and/or oxo substituents: A represents a halo-substituted benzhydryl substituent; and B represents certain specific substituted alkyl groups) and salts thereof are valuable for the treatment and prophylaxis of disorders arising from circulatory problems, especially those affecting the brain. They may be prepared by reacting a compound of formula A--M--H with a halo or acyloxy derivative corresponding to the alkyl substituent B which it is desired to introduce.Type: GrantFiled: March 14, 1988Date of Patent: July 2, 1991Assignee: Sankyo Company LimitedInventors: Koichi Hirai, Yuji Iwano, Katsumi Fujimoto, Yoshiki Matsui
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Patent number: 5026853Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: September 20, 1990Date of Patent: June 25, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4968684Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: October 10, 1989Date of Patent: November 6, 1990Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4957941Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.Type: GrantFiled: January 9, 1990Date of Patent: September 18, 1990Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4918073Abstract: A compound I ##STR1## in which R.sup.1 is cycloalkyl, alkenyl, cycloalkenyl, phenyl, ##STR2## whereJ, L, M, and E are methine or nitrogen and J', L', M', and E' are methylene, carbonyl or imino;R.sup.2 is phenyl or phenylalkyl;a is various amine radicals;m is 2, 3 or 4; andn is 1, 2, 3, or 4 is described; salts of these compounds I are also described. Compounds I and the salts are calcium antagonists.Type: GrantFiled: January 7, 1987Date of Patent: April 17, 1990Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Ruger, Hansjorg Urbach, Wilhelm Bartmann, Joachim Kaiser
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Patent number: 4908365Abstract: The present invention relates to benzhydryloxyethylpiperazine derivatives of the formula: ##STR1## It also relates to processes for the preparation of the said derivatives and pharmaceutical compositions in which they are present. The said derivatives have an antihistaminic activity without a sedative component.Type: GrantFiled: July 7, 1987Date of Patent: March 13, 1990Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
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Patent number: 4882331Abstract: The invention relates to 1-[(1,1-diphenyl)-1-alkenyl]piperazine derivatives corresponding to general formula I: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which are identical or different, represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxy group or the trifluoromethyl group; n is an integer between 1 and 3; m is an integer from 0 to 3; Z represents a hydrogen atom, a lower alkyl group or an aryl group of the formula: ##STR2## in which R.sub.6 has the same meaning as R.sub.1, R.sub.2, R.sub.3 or R.sub.4 ; and A is an oxygen atom or a group ##STR3## and to their pharmaceutically acceptable salts. Application: pharmeutical compositions with antidepressant properties.Type: GrantFiled: April 11, 1988Date of Patent: November 21, 1989Assignee: Les Laboratoires MeramInventors: Andre Buzas, Roland Ollivier
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Patent number: 4880808Abstract: A method of improving sleep in warm-blooded animals suffering from sleep disorders, which method comprises the administration of particular N-aryl-piperazinealkanamide derivatives and compositions containing the same. Novel N-aryl-piperazinealkanamide derivatives.Type: GrantFiled: March 9, 1988Date of Patent: November 14, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
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Patent number: 4874765Abstract: The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and stand for hydrogen or halogen or a trihalomethyl, lower alkyl, lower alkoxy, nitro, hydroxyl, aralkyloxy or an 1-(2-propenyl-4-piperazinyl) group;R.sub.5 stands for hydrogen or a C.sub.1-4 alkyl group;R.sub.6 represents a C.sub.3-6 alkyl, alkenyl, alkynyl group or a ##STR2## group, wherein R.sub.7 means a C.sub.2-5 alkyl, alkenyl or alkinyl group; andis 2 or 3,with the provisos that:R.sub.6 is different from isopropyl, n-butyl and isobutyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2;R.sub.6 is different from isopropyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.Type: GrantFiled: April 22, 1987Date of Patent: October 17, 1989Assignee: Richter Gedeon Vegyeszeti GyarInventors: Erzsebet Lapis, Edit Toth, Bela Kiss, Jozsef Torley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Istvan Laszlovszky
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Patent number: 4868184Abstract: The invention relates to novel benzhydryl-piperazine derivatives of the general formula (I) and the acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and stand for hydrogen or halogen, or a trihalomethyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxy group;R.sub.6 means hydrogen or a C.sub.1-4 alkyl group; andn is 2 or 3.The compounds of the general formula (I) are useful for treating diseases arising from a decrease in the dopamine level, i.e. from a hypofunction of the dopaminergic system, and have low toxicity.Type: GrantFiled: April 22, 1987Date of Patent: September 19, 1989Assignee: Richter Gedeon Vegyeszeti GyarInventors: Edith Toth, Bela Kiss, Jozsef Torley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Erzsebet Lapis, Istvan Laszlovszky
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Patent number: 4866062Abstract: The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation.In the general formula (I) ##STR1## R.sub.1 and R.sub.2 are the same or different and stand for hydrogen or halogen or a lower alkyl, trihalomethyl or lower alkoxy group.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.Type: GrantFiled: April 22, 1987Date of Patent: September 12, 1989Assignee: Richter Gedeon Vegyeszeti GyarInventors: Edit Toth, Bela Kiss, Jozsef Turley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Erzsebet Lapis, Istvan Laszlovszky
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Patent number: 4826844Abstract: Compounds of the formula: ##STR1## in which m is one of the integers 1, 2 or 3; n is one of the integers 0, 1 or 2; o is one of the integers 0, 1 or 2; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R.sub.3 is alkyl, ##STR2## where R.sub.4 and R.sub.5 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R.sub.6 is hydrogen or halo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: G. E. M. Husbands, Gary P. Stack
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Patent number: 4806685Abstract: A novel 1,1,2-triphenylpropene derivative, namely: ##STR1## acts on the endocrine system of rats. It exerts oestrogenic or antioestrogenic effects of varying strength in rats, and furthermore inhibits the growth of the mammary tumor induced by 7,12-dimethyl-benz(a)anthracene in rats.Type: GrantFiled: January 31, 1986Date of Patent: February 21, 1989Assignee: Gyogyszerkutato Inteezet/Pharmaceutical Research InstituteInventors: Gizella Abraham, Tibor Horvath, Lajos Toldy, Janos Borvendeg, Endre Csanyi, Eva Kiss, Ilona S. nee Hermann, Kalman Tory
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Patent number: 4780495Abstract: N-(substituted)-1-(piperazinealkyl)-.alpha.-(3,5-dialkyl-4-hydroxyphenyl)-. alpha.,.alpha.-disubstited acetamides, are novel compounds prepared by a novel modification of the ketoform process. The compounds are useful as stabilizers for organic materials subject to degradation in an environment in which the materials are exposed to heat, oxidation and light, particularly ultraviolet light. The compounds are especially useful in combination with known secondary stabilizers.Type: GrantFiled: January 25, 1988Date of Patent: October 25, 1988Assignee: The B. F. Goodrich CompanyInventors: John T. Lai, Pyong N. Son
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Patent number: 4757074Abstract: The present invention provides compounds of the formula (I): ##STR1## or salts, esters or amide derivatives thereof, wherein R.sub.1 is --CO.sub.2 H, --CH.dbd.CH--CO.sub.2 H, --(CH.sub.2).sub.n CO.sub.2 H, or --O--(CH.sub.2).sub.n CO.sub.2 H (n=1 to 4); R.sub.2 is C.sub.1.varies. alkyl or benzyl which is optionally substituted by a C.sub.1-4 alkyl group or groups; R.sub.3 is C.sub.1-4 alkoxy, C.sub.1-4 alkyl or halogen. Also provided are pharmaceutical formulations containing the compounds of the formula (I) and methods for the preparation of the compounds. The above mentioned compounds have antihistaminic activity.Type: GrantFiled: February 24, 1986Date of Patent: July 12, 1988Assignee: Burroughs Wellcome Co.Inventors: Geoffrey G. Coker, John W. A. Findlay
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Patent number: 4745191Abstract: The compounds ##STR1## in which R.sup.1 is 3-hydroxy, 4-hydroxy, 3-methoxy, 4-methoxy or 3,4-methylenedioxy; n is 1 or 2; and R.sup.2 is ##STR2## where R.sup.3 is hydrogen, alkoxy of 1 to 6 carbon atoms, halo or trifluoromethyl; or a pharmaceutically acceptable salt thereof possess anxiolytic and antidepressant activity and are useful in treating psychiatric disorders involving anxiety and/or depression.Type: GrantFiled: September 30, 1987Date of Patent: May 17, 1988Assignee: American Home Products CorporationInventor: G. E. Morris Husbands
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Patent number: 4618611Abstract: The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.Type: GrantFiled: December 27, 1983Date of Patent: October 21, 1986Assignee: Richter Gedeon Vegyeszeti Gyar RtInventors: Edit Toth, Jozsef Torley, Gyorgy Fekete, Laszlo Szporny, Laszlo Vereczkey, Eva Palosi, Imre Klebovich, Pal Vittay, Sandor Gorog, Istvan Hajdu
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Patent number: 4504663Abstract: The present invention concerns novel heterocyclic aminoalcoyl derivatives having the formula: ##STR1## wherein n=1, 2 or 3; A represents a nitrogen atom or the CH group, X=CH.sub.2 or CH.sub.2 O; R represents a phenyl nucleus possibly substituted; NR.sub.1 R.sub.2 =amino, methylamino, N,N-dialkylamino or an heterocyclic radical; and R.sub.3 =H, halogen, alkyl, alkyloxy or methoxy.These derivatives are useful as drugs, especially as analgesics and antidepressants.Type: GrantFiled: November 15, 1983Date of Patent: March 12, 1985Assignee: Delalande S.A.Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
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Patent number: 4476129Abstract: The invention relates to new piperazine derivatives of the general formula ##STR1## in which R' and R.sup.2 each represents 1, 2 or 3 halogen atoms, which may be the same or different,R.sup.3 represents a hydrogen atom or 1, 2 or 3 halogen atoms, X represents a hydroxy, C.sub.1-4 alkoxy, phenylcarbamoyloxy or C.sub.1-4 alkylcarbamoyloxy group,Y represents a hydrogen atom or a C.sub.1-3 alkyl group, or X and Y together with the carbon atom to which they are linked represent a carbonyl group,m is 1, 2 or 3,n is 0 or 1, with the proviso that m+n is at most 3, and their acid addition and quaternary ammonium salts.Other features of the invention areprocesses for the preparation of compounds of formula I,pharmaceutical preparations comprising a compound of formula I.Type: GrantFiled: June 29, 1983Date of Patent: October 9, 1984Assignee: Gist-Brocades N.V.Inventors: Johan Gootjes, Hendricus H. van de Kamp
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Patent number: 4431851Abstract: The present invention concerns compounds of the formula ##STR1## wherein n=1, 2 or 3; and R' represents phenyl or orthofluorophenyl. Said compounds are used as intermediates in the preparation of heterocyclic aminoalkyl derivatives which are useful as analgesics and antidepressants.Type: GrantFiled: March 8, 1983Date of Patent: February 14, 1984Assignee: Delalande S.A.Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
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Patent number: 4372975Abstract: The invention relates to new substituted 2-benzoyl-4-chloroglycinanilide derivatives, to a process for their production and to their use as medicaments.The new derivatives according to the invention correspond to the general formula ##STR1## in which: R may be a linear or branched alkyl group, preferably a lower alkyl group;R.sub.1 and R.sub.2 may be the same or different and are selected from hydrogen, alkyl, alkenyl, alkynyl, hydroxy alkyl, alkoxy alkyl and aralkyl groups, these various groups optionally being linear or branched, and from 3- to 6-membered cycloalkyl groups optionally substituted on the .alpha.-carbon atom by an alkynyl radical;in addition, the groups R.sub.1 and R.sub.Type: GrantFiled: October 27, 1980Date of Patent: February 8, 1983Assignee: Pierre Fabre SAInventors: Gilbert Mouzin, Henri Cousse, Antoine Stenger, Sylvano Casadio
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Patent number: 4348505Abstract: A liquid adduct is prepared from the reaction of an amine, a polyepoxide compound with a functionality greater than 2, and, optionally, a diglycidyl ether of bisphenol A and/or the hydrogenated equivalent thereof, an accelerator or a suitable solvent; said reaction continuing until no active epoxy groups are available. The adducts are useful as curing agents for epoxy resins in both room temperature and heat cured applications to produce protective coatings of superior properties.Type: GrantFiled: November 28, 1980Date of Patent: September 7, 1982Assignee: Ciba-Geigy CorporationInventors: Marianne Di Benedetto, John A. Gannon
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Patent number: 4289770Abstract: New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.Type: GrantFiled: June 13, 1980Date of Patent: September 15, 1981Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin
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Patent number: 4265894Abstract: Piperazine derivatives of the general formula ##STR1## wherein R.sub.1 -R.sub.9 are the same or different and each represents a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, n is 2 or 3 and X represents a group (CH.sub.2).sub.m (in which m is 1, 2, 3 or 4) or a group --CH.sub.2 --CH.dbd.CH--, having methylene linked to the piperazine group, and acid addition and quaternary ammonium salts thereof, are described.The compounds exhibit a strong specific dopaminergic activity.Also described are methods for their preparation and use as therapeutic agents in the form of therapeutic compositions.Type: GrantFiled: November 1, 1979Date of Patent: May 5, 1981Assignee: Gist Brocades, N.V.Inventor: Johan Gootjes
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Patent number: 4235896Abstract: Compounds of the formula ##STR1## in which A is lower alkyl, or a substituted or unsubstituted phenyl, thienyl, furyl, indolyl or thiaindolyl radical, R, X.sub.4 and X.sub.5 are hydrogen or lower alkyl, Y is hydrogen, hydroxy, etherified hydroxy, substituted amino, or N-attached heterocyclyl, X.sub.0 is O or OCH.sub.2 CH.sub.2 O, R' represents hydrogen, lower alkyl or acetyl; and acid-addition salts thereof, are novel and useful in pharmacy as hypolipaemiant, hypocholosterolaemiant and cholagogic agents or in the preparation of such agents.Type: GrantFiled: October 28, 1977Date of Patent: November 25, 1980Assignee: Orchimed S.A.Inventor: Andre Mieville
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Patent number: 4202896Abstract: Piperazine derivatives of the general formula ##STR1## wherein R.sub.1 -R.sub.9 are the same or different and each represents a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, n is 2 or 3 and X represents a group (CH.sub.2).sub.m (in which m is 1, 2, 3 or 4) or a group --CH.sub.2 --CH.dbd.CH--, having methylene linked to the piperazine group, and acid addition and quaternary ammonium salts thereof, are described.The compounds exhibit a strong specific dopaminergic activity.Also described are methods for their preparation and use as therapeutic agents in the form of therapeutic compositions.Type: GrantFiled: December 14, 1977Date of Patent: May 13, 1980Assignee: Gist-Brocades N.V.Inventor: Johan Gootjes
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Patent number: RE31237Abstract: New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.Type: GrantFiled: February 19, 1982Date of Patent: May 10, 1983Assignee: Pierre Fabre S.A.Inventors: Henri Cousse, Gilbert Mouzin