Chalcogen Bonded Directly To The Carbon Patents (Class 544/397)
  • Patent number: 11365195
    Abstract: 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: Grant
    Filed: November 12, 2018
    Date of Patent: June 21, 2022
    Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Amy Hauck Newman, JoLynn Barbara Giancola, Rachel D. Slack
  • Patent number: 8394954
    Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.
    Type: Grant
    Filed: March 26, 2008
    Date of Patent: March 12, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Bandari Rajendra Prasad
  • Publication number: 20120277250
    Abstract: 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: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
  • Publication number: 20100174074
    Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.
    Type: Application
    Filed: March 26, 2008
    Publication date: July 8, 2010
    Inventors: Ahmed Kamal, Bandari Rajendra Prasad
  • Patent number: 7524846
    Abstract: 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: Grant
    Filed: October 12, 2004
    Date of Patent: April 28, 2009
    Assignee: Wyeth
    Inventor: Paige Erin Mahaney
  • Patent number: 7491723
    Abstract: 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: Grant
    Filed: October 12, 2004
    Date of Patent: February 17, 2009
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, William Jay Moore, Joseph Peter Sabatucci
  • Patent number: 7419980
    Abstract: 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: Grant
    Filed: October 12, 2004
    Date of Patent: September 2, 2008
    Assignee: Wyeth
    Inventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
  • Patent number: 7034015
    Abstract: 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: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Publication number: 20040097730
    Abstract: 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: Application
    Filed: August 1, 2003
    Publication date: May 20, 2004
    Inventors: Mary Beth Young, Philippe G. Nantermet, Harold G. Selnick, Peter D. Williams
  • Patent number: 6706745
    Abstract: 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: Grant
    Filed: May 18, 2000
    Date of Patent: March 16, 2004
    Assignee: Teijin Limited
    Inventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
  • Patent number: 6387389
    Abstract: 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: Grant
    Filed: June 30, 1999
    Date of Patent: May 14, 2002
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
  • Patent number: 6214848
    Abstract: 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: Grant
    Filed: April 30, 1999
    Date of Patent: April 10, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hitoshi Ikeda, Takashi Sohda, Hiroyuki Odaka
  • Patent number: 6130222
    Abstract: 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: Grant
    Filed: April 24, 1997
    Date of Patent: October 10, 2000
    Assignee: Astra Pharma Inc.
    Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
  • Patent number: 5962479
    Abstract: 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: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5962507
    Abstract: 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: Grant
    Filed: December 5, 1997
    Date of Patent: October 5, 1999
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
  • Patent number: 5919777
    Abstract: 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: Grant
    Filed: April 23, 1997
    Date of Patent: July 6, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Thomas Kruse Hansen, Bernd Pesche, Knud Erik Andersen
  • Patent number: 5840896
    Abstract: 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: Grant
    Filed: April 18, 1995
    Date of Patent: November 24, 1998
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Herman Van Belle, Willy Joannes Carolus Van Laerhoven
  • Patent number: 5432179
    Abstract: 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: Grant
    Filed: December 30, 1993
    Date of Patent: July 11, 1995
    Assignee: Zeria Pharmaceutical Co., Ltd.
    Inventors: Kazuhiro Kumagai, Masaaki Nagasawa, Hidenori Takahashi, Tooru Abe, Takeshi Omata, Yoshihide Segawa
  • Patent number: 5324728
    Abstract: 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: Grant
    Filed: December 2, 1991
    Date of Patent: June 28, 1994
    Assignee: Fujirebio Inc.
    Inventors: Yasuo Sekine, Tetsuaki Yamaura, Masato Nishimura, Eri Kojima, Yasuko Emoto, Yasushi Higashide
  • Patent number: 5308840
    Abstract: 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: Grant
    Filed: April 6, 1992
    Date of Patent: May 3, 1994
    Assignee: Green Cross Corporation
    Inventors: Naoki Sugiyama, Fumihiko Akaboshi, Haruko Yakumaru, Tomokazu Gotoh, Masanori Sugiura, Shigeki Kuwahara, Masahiko Kajii, Yoshiko Tanaka, Takao Kondoh, Chikara Fukaya
  • Patent number: 5276035
    Abstract: 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: Grant
    Filed: May 4, 1992
    Date of Patent: January 4, 1994
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Erling Guddal, Erik B. Nielsen
  • Patent number: 5066680
    Abstract: 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: Grant
    Filed: February 5, 1990
    Date of Patent: November 19, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
  • Patent number: 5036098
    Abstract: 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: Grant
    Filed: September 14, 1989
    Date of Patent: July 30, 1991
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Kiyoshi Kimura, Masahiro Kise, Iwao Morita
  • Patent number: 5028610
    Abstract: 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: Grant
    Filed: March 14, 1988
    Date of Patent: July 2, 1991
    Assignee: Sankyo Company Limited
    Inventors: Koichi Hirai, Yuji Iwano, Katsumi Fujimoto, Yoshiki Matsui
  • Patent number: 5026853
    Abstract: 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: Grant
    Filed: September 20, 1990
    Date of Patent: June 25, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
  • Patent number: 4968684
    Abstract: 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: Grant
    Filed: October 10, 1989
    Date of Patent: November 6, 1990
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
  • Patent number: 4957941
    Abstract: 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: Grant
    Filed: January 9, 1990
    Date of Patent: September 18, 1990
    Assignee: United Pharmaceuticals, Inc.
    Inventor: William M. Davis
  • Patent number: 4918073
    Abstract: 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: Grant
    Filed: January 7, 1987
    Date of Patent: April 17, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Wilhelm Bartmann, Joachim Kaiser
  • Patent number: 4908365
    Abstract: 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: Grant
    Filed: July 7, 1987
    Date of Patent: March 13, 1990
    Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
  • Patent number: 4882331
    Abstract: 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: Grant
    Filed: April 11, 1988
    Date of Patent: November 21, 1989
    Assignee: Les Laboratoires Meram
    Inventors: Andre Buzas, Roland Ollivier
  • Patent number: 4880808
    Abstract: 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: Grant
    Filed: March 9, 1988
    Date of Patent: November 14, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Marc G. C. Verdonck
  • Patent number: 4874765
    Abstract: 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: Grant
    Filed: April 22, 1987
    Date of Patent: October 17, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar
    Inventors: Erzsebet Lapis, Edit Toth, Bela Kiss, Jozsef Torley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Istvan Laszlovszky
  • Patent number: 4868184
    Abstract: 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: Grant
    Filed: April 22, 1987
    Date of Patent: September 19, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar
    Inventors: Edith Toth, Bela Kiss, Jozsef Torley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Erzsebet Lapis, Istvan Laszlovszky
  • Patent number: 4866062
    Abstract: 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: Grant
    Filed: April 22, 1987
    Date of Patent: September 12, 1989
    Assignee: Richter Gedeon Vegyeszeti Gyar
    Inventors: Edit Toth, Bela Kiss, Jozsef Turley, Eva Palosi, Istvan Hajdu, Laszlo Szporny, Dora Groo, Erzsebet Lapis, Istvan Laszlovszky
  • Patent number: 4826844
    Abstract: 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: Grant
    Filed: September 30, 1987
    Date of Patent: May 2, 1989
    Assignee: American Home Products Corporation
    Inventors: G. E. M. Husbands, Gary P. Stack
  • Patent number: 4806685
    Abstract: 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: Grant
    Filed: January 31, 1986
    Date of Patent: February 21, 1989
    Assignee: Gyogyszerkutato Inteezet/Pharmaceutical Research Institute
    Inventors: Gizella Abraham, Tibor Horvath, Lajos Toldy, Janos Borvendeg, Endre Csanyi, Eva Kiss, Ilona S. nee Hermann, Kalman Tory
  • Patent number: 4780495
    Abstract: 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: Grant
    Filed: January 25, 1988
    Date of Patent: October 25, 1988
    Assignee: The B. F. Goodrich Company
    Inventors: John T. Lai, Pyong N. Son
  • Patent number: 4757074
    Abstract: 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: Grant
    Filed: February 24, 1986
    Date of Patent: July 12, 1988
    Assignee: Burroughs Wellcome Co.
    Inventors: Geoffrey G. Coker, John W. A. Findlay
  • Patent number: 4745191
    Abstract: 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: Grant
    Filed: September 30, 1987
    Date of Patent: May 17, 1988
    Assignee: American Home Products Corporation
    Inventor: G. E. Morris Husbands
  • Patent number: 4618611
    Abstract: 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: Grant
    Filed: December 27, 1983
    Date of Patent: October 21, 1986
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt
    Inventors: Edit Toth, Jozsef Torley, Gyorgy Fekete, Laszlo Szporny, Laszlo Vereczkey, Eva Palosi, Imre Klebovich, Pal Vittay, Sandor Gorog, Istvan Hajdu
  • Patent number: 4504663
    Abstract: 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: Grant
    Filed: November 15, 1983
    Date of Patent: March 12, 1985
    Assignee: Delalande S.A.
    Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
  • Patent number: 4476129
    Abstract: 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: Grant
    Filed: June 29, 1983
    Date of Patent: October 9, 1984
    Assignee: Gist-Brocades N.V.
    Inventors: Johan Gootjes, Hendricus H. van de Kamp
  • Patent number: 4431851
    Abstract: 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: Grant
    Filed: March 8, 1983
    Date of Patent: February 14, 1984
    Assignee: Delalande S.A.
    Inventors: Gerard H. Moinet, Philippe L. Dostert, Guy R. Bourgery
  • Patent number: 4372975
    Abstract: 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: Grant
    Filed: October 27, 1980
    Date of Patent: February 8, 1983
    Assignee: Pierre Fabre SA
    Inventors: Gilbert Mouzin, Henri Cousse, Antoine Stenger, Sylvano Casadio
  • Patent number: 4348505
    Abstract: 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: Grant
    Filed: November 28, 1980
    Date of Patent: September 7, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Marianne Di Benedetto, John A. Gannon
  • Patent number: 4289770
    Abstract: 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: Grant
    Filed: June 13, 1980
    Date of Patent: September 15, 1981
    Assignee: Pierre Fabre S.A.
    Inventors: Henri Cousse, Gilbert Mouzin
  • Patent number: 4265894
    Abstract: 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: Grant
    Filed: November 1, 1979
    Date of Patent: May 5, 1981
    Assignee: Gist Brocades, N.V.
    Inventor: Johan Gootjes
  • Patent number: 4235896
    Abstract: 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: Grant
    Filed: October 28, 1977
    Date of Patent: November 25, 1980
    Assignee: Orchimed S.A.
    Inventor: Andre Mieville
  • Patent number: 4202896
    Abstract: 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: Grant
    Filed: December 14, 1977
    Date of Patent: May 13, 1980
    Assignee: Gist-Brocades N.V.
    Inventor: Johan Gootjes
  • Patent number: RE31237
    Abstract: 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: Grant
    Filed: February 19, 1982
    Date of Patent: May 10, 1983
    Assignee: Pierre Fabre S.A.
    Inventors: Henri Cousse, Gilbert Mouzin