The Other Ring Nitrogen Is Unsubstituted Or Alkyl Substituted Only, Or Salt Thereof Patents (Class 544/395)
  • Patent number: 4859675
    Abstract: An 1-[2-(phenylmethyl)phenyl]piperazine of the formula (I), ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl or halogen, R.sub.2 is hydrogen, C.sub.1-4 alkyl, halogen or C.sub.1-4 alkoxy and R.sub.3 is hydrogen or methyl.such compounds are useful as antidepressive agents.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: August 22, 1989
    Assignee: Ferrer Internacional S.A.
    Inventors: Rafael Foguet, Ernesto Forne, Aurelio Sacristan, Jose A. Ortiz
  • Patent number: 4855292
    Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.2 is 1-pyrrolidinyl which may have 1 to 2 substituents selected from the group consisting of (i) C.sub.1 -C.sub.6 alkyl, (ii) amino-(C.sub.1 -C.sub.6)alkyl, said amino being optionally substituted by 1 or 2 substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl, and C.sub.1 -C.sub.6 alkoxycarbonyl, (iii) amino which may be substituted by 1 or 2 substituents selected from C.sub.1 -C.sub.6 alkyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, and C.sub.1 -C.sub.6 alkanoyl, and (iv) 2-oxo-1,3-dioxolenemethylamino which is substituted by C.sub.1 -C.sub.6 alkyl; or 1-piperidinyl which may have 1 to 3 substituents selected from oxo, hydroxy, halogen and C.sub.1 -C.sub.6 alkyl, and R.sup.3 is C.sub.1 -C.sub.
    Type: Grant
    Filed: July 23, 1987
    Date of Patent: August 8, 1989
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hiraki Ueda, Hisashi Miyamoto, Shinji Aki, Tatsuya Otsuka
  • Patent number: 4843070
    Abstract: Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.
    Type: Grant
    Filed: May 13, 1987
    Date of Patent: June 27, 1989
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masahiro Kise, Masahiko Kitano, Masakuni Ozaki, Kenji Kazuno, Ichiro Shirahase, Yoshifumi Tomii, Jun Segawa
  • Patent number: 4833247
    Abstract: A process for the production of 2-benzyl fatty acids and esters thereof corresponding to the following formula ##STR1## comprising reacting 2-fatty alkyl-4,4-dimethyl-2-oxazolines with benzaldehydes corresponding to the formula R.sup.2 --C.sub.6 H.sub.4 --CHO to form 2-(1-benzylidene)-fatty alkyl-4,4-dimethyl-2-oxazolines, catalytically hydrogenating the products of this reaction to the 2-(1-benzyl)-fatty alkyl-4,4-dimethyl oxazolines and converting the products thus formed by acid-catalyzed hydrolysis or solvolysis with an alcohol of the formula R.sup.5 OH into the 2-benzyl fatty acids or esters thereof. Amidosulfonic acid gives particularly high yields as catalyst for the reaction of the 2-fatty alkyl-4,4-dimethyl-2-oxazolines with the benzaldehydes.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: May 23, 1989
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventor: Horst-Juergen Krause
  • Patent number: 4826975
    Abstract: The invention is concerned with fused cycloaliphatic aminoalcohols having pharmacological activity as anti-hypertensive, platelet aggregation inhibiting, hypolipemic, antianoxic and spasmolytic activity. The compounds have the generic formula ##STR1## in which the symbol n is an integer selected from 1 to 2, the compounds pertaining therefore to the indanol and tetralol series.
    Type: Grant
    Filed: December 10, 1986
    Date of Patent: May 2, 1989
    Assignee: Maggioni-Winthrop S.P.A.
    Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
  • Patent number: 4774336
    Abstract: N,N'-dialkylpiperazines are prepared by contacting ethylene glycol and a primary amine in the presence of a homogeneous ruthenium-phosphine catalyst. For example, ethylene glycol and aniline are reacted in the presence of ruthenium trichloride and triphenylphosphine to produce N,N'-diphenylpiperazine.
    Type: Grant
    Filed: October 2, 1986
    Date of Patent: September 27, 1988
    Assignee: Texaco Inc.
    Inventor: Wei-Yang Su
  • Patent number: 4699910
    Abstract: The compound of the formula ##STR1## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compound as well as its salts are useful as analgesics.
    Type: Grant
    Filed: November 22, 1985
    Date of Patent: October 13, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Herbert Merz, Klaus Stockhaus, Hans M. Jennewein
  • Patent number: 4656267
    Abstract: The synthesis of substituted 2(1H)-quinazolinone-1-alkanoic acids and their esters is described. The novel quinazolinones are renal vasodilators and as such reduce vascular resistance to renal blood flow. The quinazolinones are useful as cardiovascular agents.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: April 7, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Seymour D. Levine, Dennis M. Mulvey, Alfonso J. Tobia
  • Patent number: 4616086
    Abstract: The present invention is concerned with new carboxylic acid derivatives, with processes for the preparation thereof and with pharmaceutical compositions for lipid depression and thrombocyte aggregation, containing them, and to methods for treating infirmaties caused by excess lipids or thrombocyte aggregation.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: October 7, 1986
    Assignee: Boehringer Mannheim GmbH
    Inventors: Ernst-Christian Witte, Hans P. Wolff, Bernd Hagenbruch, Karlheinz Stegmeir, Johannes Pill
  • Patent number: 4597912
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 independently of one another are unsubstituted or hydroxy substituted, C.sub.1 -C.sub.4 alkoxy substituted, cyano substituted, C.sub.1 -C.sub.4 alkoxycarbonyl substituted, di-C.sub.1 -C.sub.4 alkylamino substituted, (CH.sub.3)(C.sub.6 H.sub.5 CH.sub.2)NC.sub.2 H.sub.4 substituted, chlorine substituted or bromine substituted C.sub.1 -C.sub.4 -alkyl, cyclohexyl, benzyl, phenylethyl or phenyl, R.sup.1 and R.sup.2 together with the nitrogen are morpholino, pyrrolidino, piperidino or N-methylpiperazino;R.sup.3 is hydrogen, chlorine, bromine, methyl, ethyl, methoxy, ethoxy or nitro;R.sup.4 and R.sup.5 independently of one another are hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl; X is oxygen or imino; A.sup.
    Type: Grant
    Filed: May 17, 1985
    Date of Patent: July 1, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Manfred Eisert, Klaus Grychtol
  • Patent number: 4544657
    Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.
    Type: Grant
    Filed: May 19, 1983
    Date of Patent: October 1, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Richard W. Kierstead, John G. Mullin, Jr., Keiji Nakamura, Mitsuru Tateishi, Teitel Sidney, Jay P. O'Brien
  • Patent number: 4518712
    Abstract: An analgesic composition containing as active ingredient a piperazine derivative represented by the general formula (1) ##STR1## wherein R.sub.1 represents a cyclopropylmethyl group, an isopropyl group or an allyl group and R.sub.2 represents a phenyl group having as substituent a halogen atom or a trifluoromethyl group.
    Type: Grant
    Filed: June 22, 1981
    Date of Patent: May 21, 1985
    Assignee: Taiho Pharmaceutical Company Limited
    Inventors: Hajime Fujimura, Yasuzo Hiramatsu, Tomio Yamazaki, Shozo Yamada, Takaji Honna
  • Patent number: 4515793
    Abstract: A compound of the formula ##STR1## in which A is ##STR2## n is 1, 2 or 3, and R is phenyl optionally substituted with halogen, alkyl, phenyl, cyano, hydroxy, alkoxy, mercapto, sulfinyl, sulfonyl, amino, nitro, trifluoromethyl and/or naphthyl radicals; or a furan, thiophene, pyridine, benzofuran, dibenzothiophene or thianthrene radical,or a pharmacologically acceptable salt thereof, for treating schistosomiasis.
    Type: Grant
    Filed: July 27, 1983
    Date of Patent: May 7, 1985
    Assignee: Edna McConnell Clark Foundation
    Inventors: Leslie M. Werbel, Norman Colbry, William Turner, Donald F. Worth
  • Patent number: 4504660
    Abstract: 2,6-Diaminobenzonitriles, useful in the production of N-(2-cyano-3-substituted or unsubstituted amino-phenyl)oxamate and N-(2-cyano-3-substituted or unsubstituted amino-phenyl)tetrazole-5-carboxamide antiallergy and antisecretory agents, are prepared by sequential displacement of the fluoro substituents from 2,6-difluorobenzonitrile with the appropriately substituted amine.
    Type: Grant
    Filed: July 6, 1982
    Date of Patent: March 12, 1985
    Assignee: American Home Products Corporation
    Inventors: Dieter H. Klaubert, Stanley C. Bell
  • Patent number: 4487721
    Abstract: The present invention is directed to a process for producing 2-amino-2-arylacetonitriles of general formula I: ##STR1## wherein R and R.sup.1 independently represent hydrogen, hydroxy, hydroxy(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.6)alkyl, 2-furyl, 2-thienyl, 4-pyridinyl, 1-pyrrolydinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-phenylpiperazinyl, or phenyl which can optionally be substituted with from 1 to 3 substituents independently selected from (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy, or R and R.sup.1 independently represent a phenyl(C.sub.1 -C.sub.4)alkyl or a phenyl(C.sub.1 -C.sub.4)alkoxy group wherein the phenyl group can be either unsubstituted or substituted as above.An arylaldehyde derivative of formula II ##STR2## is reacted with chloroform in base and in the presence of ammonia to give the 2-amino-2-arylacetonitrile derivative.
    Type: Grant
    Filed: June 7, 1983
    Date of Patent: December 11, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventor: Romeo Ciabatti
  • Patent number: 4486429
    Abstract: Compounds of the formula I: ##STR1## in which R represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms and R.sub.1 and R.sub.2, which may be identical or different independently represent a hydrogen atom, an alkyl radical containing from 1 to 4 carbon atoms, a --CONH.sub.2 radical, a --CO.sub.2 alk.sub.1 radical in which alk.sub.1 represents an alkyl radical containing from 2 to 8 carbon atoms, or an--SO.sub.2 alk.sub.2 radical in which alk.sub.2 represents an alkyl radical containing from 1 to 8 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom form a heterocycle provided that R.sub.1 and R.sub.2 are not both hydrogen, as well as the alkali metal, alkaline earth metal, ammonium or amine salts of compounds of formula I in which R represents a hydrogen atom. These compounds are useful in treating hyperchlorhydria, gastric or gastroduodenal ulcers, gastritis, hiatal hernias and gastric or gastroduodenal ailments accompanied by gastric hyperacidity.
    Type: Grant
    Filed: October 20, 1982
    Date of Patent: December 4, 1984
    Assignee: Roussel Uclaf
    Inventors: Mario Bianchi, Fernando Barzaghi
  • Patent number: 4477666
    Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
    Type: Grant
    Filed: February 12, 1982
    Date of Patent: October 16, 1984
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
  • Patent number: 4438268
    Abstract: This invention relates to new nematic liquid crystal substances for electro-optical components.The object of this invention is to create substances for electro-optical components combining chemical and thermal stability with low melting and high clear points at low operational voltage, as well as to processes for their production.It has been found that new liquid-crystal trans-6-n-alkyl-decalin-2-carbonic acid ester of the general formula ##STR1## can be introduced into electro-optical components. These substances are produced by the catalytic high-pressure hydrogenation of 6-n-alkylnaphthalene-2-carbonic acids, separation of the trans-isomers by distillation, and esterification with the corresponding hydroxy compounds of the acyl chlorides obtained through reaction with thionyl chloride.
    Type: Grant
    Filed: September 14, 1981
    Date of Patent: March 20, 1984
    Inventors: Horst Zaschke, Wolfgang Schafer, Hans-Joachim Deutscher, Dietrich Demus, Gerhard Pelzl
  • Patent number: 4435399
    Abstract: A series of novel 2-aryl-1-(imidazol-1-yl)-8-(4-piperazin-1-ylphenoxy)octan-2-ol derivatives has been prepared, including their pharmaceutically acceptable acid addition salts. These particular compounds are useful in therapy as antifungal agents for the treatment of various topical, mucosal and systemic fungal infections in animals, including humans. Preferred member compounds include 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-ethylpiperazin-1-yl)phenoxy] octan-2-ol, 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-(4-n-propylpiperazin-1-yl)ph enoxy]octan-2-ol and 2-(2,4-dichlorophenyl)-1-(imidazol-1-yl)-8-[4-(4-isopropylpiperazin-1-yl)p henoxy]octan-2-ol, respectively. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: June 25, 1982
    Date of Patent: March 6, 1984
    Assignee: Pfizer Inc.
    Inventors: Kenneth Richardson, Geoffrey E. Gymer
  • Patent number: 4404215
    Abstract: This invention relates to novel arylethanol and to process for producing the said compounds.The arylethanols of the invention have valuable pharmacological properties and find a use in human or animal therapy.
    Type: Grant
    Filed: November 18, 1981
    Date of Patent: September 13, 1983
    Assignee: Science Union et Cie
    Inventors: Michel Vincent, Georges Remond, Jacques Bure
  • Patent number: 4367339
    Abstract: There are provided di- tri- and tetrasubstituted N-nitroaniline compounds and inorganic and organic salts thereof which are effective for increasing axillary branching, improving canopy and enhancing flowering of herbaceous ornamental plants and graminaceous crops, leguminous crops, cotton and sunflowers. The salts are also effective as yield enhancing agents and lodging inhibitors for the crops.
    Type: Grant
    Filed: August 18, 1980
    Date of Patent: January 4, 1983
    Assignee: American Cyanamid Company
    Inventors: Thomas D. O'Neal, Prithvi R. Bhalla, Barrington Cross
  • Patent number: 4342756
    Abstract: Compounds are described of the formula ##STR1## (and their salts and solvates) in which: X is cis or trans --CH.dbd.CH--;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.3 where R.sup.3 is H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl;Y is a saturated heterocyclic amino group having 5-8 ring members; andR.sup.2 is C.sub.2-4 alkanoyl, C.sub.3-6 alkenyl (optionally substituted), C.sub.1-12 alkyl, or substituted or unsubstituted phenylalkyl, biphenylalkyl or naphthylalkyl.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and anti-asthmatic agents.
    Type: Grant
    Filed: April 29, 1981
    Date of Patent: August 3, 1982
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw, Norman F. Hayes
  • Patent number: 4335124
    Abstract: The compounds are 4-phenyl-4-lower alkyl-substituted-3-buten-2-ones, and -2-halo-1,3-butadienes, e.g., 2-(p-biphenylyl)-2-penten-4-one, and are useful as pharmaceuticals.
    Type: Grant
    Filed: October 14, 1980
    Date of Patent: June 15, 1982
    Assignee: Sandoz, Inc.
    Inventor: Eugene E. Galantay
  • Patent number: 4273787
    Abstract: The compounds are 4-phenyl-4-lower alkyl-substituted-3-buten-2-ones, and -2-halo-1,3-butadienes, e.g., 2-(p-biphenylyl)-2-penten-4-one, and are useful as pharmaceuticals.
    Type: Grant
    Filed: August 9, 1979
    Date of Patent: June 16, 1981
    Assignee: Sandoz, Inc.
    Inventor: Eugene E. Galantay
  • Patent number: 4266080
    Abstract: Perfluoroalkyl compounds containing ether groups have the formulaR.sub.f R.sub.1 SCH.sub.2 CH.sub.2 O T Zwherein R.sub.f is a perfluoroalkyl, R.sub.1 is alkylene or alkyleneoxy or aminoalkylene, T is alkylene, and Z is hydrogen; hydroxy; NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 each is alkyl or together with nitrogen form a heterocyclic ring; N.sup.+ R.sub.3 R.sub.4 (R.sub.5)X.sub.z.sup.-y, where R.sub.5 is hydrogen, oxide, alkyl, or substituted alkyl, X is an anion, and y is 1 or 2; z is 0 or 1 or is --OCH.sub.2 CH.sub.2 SR.sub.1 R.sub.f ; can be prepared directly by free-radical catalyzed addition of a perfluoroalkylthiol to a vinyl ether or subsequent reaction. These compounds are useful as surfactants and oil spill collecting agents.
    Type: Grant
    Filed: February 2, 1978
    Date of Patent: May 5, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert A. Falk, Karl F. Mueller
  • Patent number: 4228105
    Abstract: A process for the production of compounds of formula I, ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms,R.sub.2 is hydrogen, fluorine, chlorine or bromine, andR.sub.3 is bromine, iodine, isobutyl, tert. butyl, cyclohexyl, cyclohexenyl; or phenyl, optionally substituted by fluorine, chlorine, bromine or alkoxy of 1 to 4 carbon atoms; or a radical of formula II, ##STR2## in which either R.sub.4 and R.sub.5 are the same or different and each signifies alkyl of 1 to 3 carbon atoms,orR.sub.4 and R.sub.5 together signify the radical --(CH.sub.2).sub.n --, in which n is 4 or 5, the radical --CH.sub.2 --CH.sub.2 --0--CH.sub.2 --CH.sub.2 --, the radical --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, or the radical --CH.sub.2 --CH.sub.2 --N(R.sub.6)--CH.sub.2 --CH.sub.2 --, in which R.sub.6 is hydrogen or alkyl of 1 to 3 carbon atoms. Hydroxyketone and hydroxy imine intermediates are also disclosed.The compounds of formula I are known to exhibit anti-inflammatory activity.
    Type: Grant
    Filed: November 27, 1978
    Date of Patent: October 14, 1980
    Assignee: Sandoz Ltd.
    Inventor: Rudiger Jeck
  • Patent number: 4223144
    Abstract: Compounds of the general formula I ##STR1## where B is a bridge member,the radicals R independently of one another are hydrogen or substituted or unsubstituted alkyl, or two radicals R together with the nitrogen are a heterocyclic saturated 5-membered or 6-membered ring,the radicals R.sup.1 independently of one another are hydrogen or C.sub.1 -C.sub.4 -alkyl,the radicals R.sup.2 independently of one another are hydrogen, C.sub.1 -C.sub.4 -alkyl or halogen,the radicals R.sup.3 independently of one another are hydrogen or substituted or unsubstituted alkyl or together are an alkylene group, and X.crclbar. is an anion. The compounds of the formula I are particularly suitable for dyeing paper.
    Type: Grant
    Filed: September 5, 1978
    Date of Patent: September 16, 1980
    Assignee: BASF Aktiengesellschaft
    Inventors: Hellmut Kast, Klaus Grychtol, Franz Feichtmayr
  • Patent number: 4210646
    Abstract: Novel antimicrobial compositions comprising a 1-(aryloxyphenyl)piperazine as an active ingredient and a method of combatting the growth of microorganisms by the use of such 1-(aryloxyphenyl)piperazines.
    Type: Grant
    Filed: April 11, 1978
    Date of Patent: July 1, 1980
    Assignee: Janssen Pharmaceutica N.V.
    Inventor: Marcel A. C. Janssen
  • Patent number: 4153609
    Abstract: A 3-indolyl-3-bis-aminophenyl-phthalide compound of the formula ##STR1## wherein R.sub.1 represents alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, cycloalkyl, or unsubstituted or substituted phenyl or benzyl wherein the substituents are halogen, nitro, lower alkyl or lower alkoxy,R.sub.2 represents hydrogen, alkyl which has at most 12 carbon atoms and is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, cycloalkyl, or benzyl which is unsubstituted or substituted by halogen, nitro, lower alkyl or lower alkoxy, orR.sub.1 and R.sub.2 together with the nitrogen atom linking them represent a 5- or 6-membered heterocyclic radical,X.sub.1 and X.sub.2 independently of one another represent hydrogen, lower alkyl, cycloalkyl, benzyl which is unsubstituted or substituted by halogen, nitro, lower alkyl or lower alkoxy, or acyl having 1 to 8 carbon atoms, and X.sub.
    Type: Grant
    Filed: January 10, 1977
    Date of Patent: May 8, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean C. Petitpierre, Robert Garner
  • Patent number: 4139621
    Abstract: 1-(3,5-Dichlorophenyl)piperazines bearing a fluoro, chloro, methyl, nitro, hydroxy, methoxy, cyano, amino, methylamino or dimethylamino substituent in the 4-position of the phenyl ring and being further optionally substituted in the 4-position of the piperazine ring by tetrahydropyranyl, alkyl, formyl, carboxy, alkanoyl or carboalkoxy, and the acid addition salts thereof, are tranquilizers. A typical embodiment is 1-(3,4,5-trichlorophenyl)piperazine hydrochloride.
    Type: Grant
    Filed: December 5, 1977
    Date of Patent: February 13, 1979
    Assignee: Beecham Group Limited
    Inventors: Derek V. Gardner, Alexander C. Goudie
  • Patent number: 4127658
    Abstract: Disclosed are compounds of the class 1-phenyl-2,3-butadien-1-ol e.g. 2-(p-biphenylyl)-3,4-pentadien-2-ol, which are useful by reason of their pharmacological activity in animals, e.g., as anti-inflammatory agents and tranquilizers. Said compounds can be prepared, e.g., by reduction of a corresponding 4-substituted-1-phenyl-2-butyne-1-ol with a complex hydride such as lithium aluminum hydride.
    Type: Grant
    Filed: March 23, 1978
    Date of Patent: November 28, 1978
    Assignee: Sandoz, Inc.
    Inventor: Eugene E. Galantay
  • Patent number: 4126691
    Abstract: New .alpha.-(cyclic tert. aminophenyl)-aliphatic acids, e.g. those of the formula ##STR1## AND FUNCTIONAL DERIVATIVES THEREOF, ARE ANTI-INFLAMMATORY AGENTS.
    Type: Grant
    Filed: December 6, 1976
    Date of Patent: November 21, 1978
    Assignee: Ciba-Geigy Corporation
    Inventors: Richard W. J. Carney, George DEStevens
  • Patent number: 4113866
    Abstract: Novel compounds of the formula: ##STR1## wherein R.sub.1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH.sub.2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R.sub.2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R.sub.5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R.sub.
    Type: Grant
    Filed: April 1, 1977
    Date of Patent: September 12, 1978
    Assignee: The Upjohn Company
    Inventor: Daniel Lednicer
  • Patent number: 4094980
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are chlorine, orR.sub.1 is methyl and R.sub.2 is methoxy,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anti-hyperlipidemics and anti-hypercholesteremics with practically negligible CNS-depressing side effects.
    Type: Grant
    Filed: December 10, 1976
    Date of Patent: June 13, 1978
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Ernst-Otto Renth, Anton Mentrup, Kurt Schromm, Wilhelm Frolke
  • Patent number: 4093446
    Abstract: Compounds of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group,Y is a hydrogen atom, a halogen atom, or a trihalomethyl group, andZ is a substituted alkoxy group,And compositions containing these compounds exhibit herbicidal activity.
    Type: Grant
    Filed: August 31, 1976
    Date of Patent: June 6, 1978
    Assignee: Rohm and Haas Company
    Inventors: Horst O. Bayer, Colin Swithenbank, Roy Y. Yih
  • Patent number: 4091101
    Abstract: 6-(1-Piperazinyl)quinoxaline and pharmaceutically acceptable salts thereof have serotoninmimetic activity. It is prepared by reducing the nitro group of 1-(3-amino-4-nitrophenyl)piperazine followed by treatment with glyoxal.
    Type: Grant
    Filed: June 15, 1977
    Date of Patent: May 23, 1978
    Assignee: Merck & Co., Inc.
    Inventors: William C. Lumma, Jr., Walfred S. Saari