The Additional Hetero Ring Is Five-membered Patents (Class 544/152)
  • Patent number: 5196532
    Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: March 23, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
  • Patent number: 5194608
    Abstract: A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: March 16, 1993
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tatsuo Toyoda, Toshihiro Fujioka, Kunio Hayashi, Masuhisa Nakamura, Naofumi Hashimoto
  • Patent number: 5189035
    Abstract: The invention provides furanone derivatives of the general formula ##STR1## in which R.sup.1 represents a halogen atom or an optionally substituted alkyl or alkoxy group, R.sup.2 represents a halogen atom or an optionally substituted alkyl, aryl or heterocyclyl group, R.sup.7 represents a C.sub.1-4 alkyl group and Q represents an optionally substituted morpholino or amino group; processes for their preparation; compositions containing such compounds and their use as fungicides.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: February 23, 1993
    Assignee: Shell Research Limited
    Inventors: Jurgen Curtze, Guido Albert
  • Patent number: 5177095
    Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
  • Patent number: 5145975
    Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: September 8, 1992
    Assignee: The Rockefeller University
    Inventors: Graeme B. Henderson, Peter C. Ulrich, Anthony Cerami
  • Patent number: 5128348
    Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Gregory S. Basarab
  • Patent number: 5104869
    Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: April 14, 1992
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Charles Frederick, Jeremy I. Levin, Fuk-Wah Sum, Marvin F. Reich
  • Patent number: 5091426
    Abstract: A method of preventing epileptic seizures in a human or lower animal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: ##STR1## wherein (a) X is halo or nil, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and(b) R is R.sup.1 C(O)OH, R.sup.1 C(O)N(R.sup.2).sub.2, or R.sup.1 N(R.sup.2).sub.2 ; whereR.sup.1 is C.sub.1 -C.sub.3 alkylene which is unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl; andeach R.sup.2 is, independently, hydrogen or lower alkyl; orboth R.sup.2 groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms, wherein one of which is nitrogen and the other is selected from oxygen and nitrogen and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl;or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: February 25, 1992
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventor: Stanford S. Pelosi, Jr.
  • Patent number: 5081147
    Abstract: Compounds of the formula ##STR1## where R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1 *, CO--O--R.sub.1 *, CO--NH--R.sub.1 *, or PO(OR.sub.1 *).sub.2, PO(OR.sub.1 *)R.sub.1 * where R.sub.1 * independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl;R.sub.2 is H or alkyl of 1 to 20 carbons;X is H, R.sub.3, CO--R.sub.3, CO--O--R.sub.3, CO--NH--R.sub.3, CO--N--(R.sub.3).sub.2, PO(OR.sub.3).sub.2, PO(OR.sub.3)R.sub.3, and R.sub.3 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy or with a COR.sub.3 * group where R.sub.3 * is H, lower alkyl, OH, OR.sub.3 **, NH.sub.2, NHR.sub.3 ** or N(R.sub.3 **).sub.2 group wherein R.sub.3 ** independently is H or lower alkyl, with the proviso that when X is CO--O--R.sub.3 or is CO--NH--R.sub.3 then R.sub.3 is not hydrogen;Y is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.
    Type: Grant
    Filed: March 15, 1990
    Date of Patent: January 14, 1992
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 5075301
    Abstract: A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with gastrointestinal dyskinesia.
    Type: Grant
    Filed: August 14, 1990
    Date of Patent: December 24, 1991
    Assignee: Kyowa Hakko Kogyo, Co., Ltd.
    Inventors: Setsuya Sasho, Shunji Ichikawa, Hiromasa Kato, Hiroyuki Obase, Katsuichi Shuto, Yoshimasa Oiji
  • Patent number: 5053504
    Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.
    Type: Grant
    Filed: November 29, 1989
    Date of Patent: October 1, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5047406
    Abstract: Substituted cyclohexanols and cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
    Type: Grant
    Filed: May 2, 1990
    Date of Patent: September 10, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Bradley W. Caprathe, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
  • Patent number: 5023272
    Abstract: A method of preventing epileptic seizures in a human or mammal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: ##STR1## wherein (a) X is halo or hydrogen, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and(b) R is N(R.sup.3).sub.2, OR.sup.1 N(R.sup.3).sub.2, N(R.sup.2)R.sup.1 N(R.sup.3).sub.2, or N(R.sup.2)N(R.sup.3).sub.2 ; whereR.sup.1 is C.sub.1 -C.sub.3 alkylene which is unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl;R.sup.2 is hydrogen or lower alkyl; andeach R.sup.3 is, independently, hydrogen or lower alkyl; or both R.sup.
    Type: Grant
    Filed: June 23, 1989
    Date of Patent: June 11, 1991
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Homer A. Burch, Alan W. Castellion, Stanford S. Pelosi, Jr.
  • Patent number: 4996203
    Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.
    Type: Grant
    Filed: June 8, 1989
    Date of Patent: February 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
  • Patent number: 4988727
    Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: January 29, 1991
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Michel Fortin
  • Patent number: 4987132
    Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: January 22, 1991
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
  • Patent number: 4959362
    Abstract: An ascorbic acid derivative of the formula: ##STR1## wherein R.sup.1 is organic residue having molecular weight of from 15 to 700, R.sup.2 is hydrogen or hydroxyl, R.sup.3 is hydrogen, acyl, optionally substituted phosphono or sulfo, and R.sup.3 and hydroxyl or R.sup.2 may form acetal residue or ketal residue, and a salt thereof are provided.The compound [I] and salts thereof have antioxidant activity and excellent prophylactic and improving actions on disorders of circulatory functions, and they are usefule as antioxidant agent for food and as agents of prophylaxis and improvement of circulatory functional disorders.
    Type: Grant
    Filed: September 19, 1988
    Date of Patent: September 25, 1990
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Shinji Terao, Minoru Hirata
  • Patent number: 4958043
    Abstract: A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: September 18, 1990
    Assignee: Eastman Kodak Company
    Inventors: Max A. Weaver, Wayne P. Pruett, Samuel D. Hilbert
  • Patent number: 4957917
    Abstract: New furanone compounds have anti-inflammatory, immunosuppressive and anti-proliferative activity and are useful in treating psoriasis and modifying calcium homeostasis. A compound of the invention is 4-[1-acetoxy-2-N-(dodecyl) amidoethyl]-5-hydroxy-2(5H)-furanone.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: September 18, 1990
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 4942170
    Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.
    Type: Grant
    Filed: May 27, 1988
    Date of Patent: July 17, 1990
    Assignee: The Rockefeller University
    Inventors: Graeme B. Henderson, Peter C. Ulrich, Anthony Cerami
  • Patent number: 4904656
    Abstract: Fungicidally active 2-aminomethyltetrahydrofurans of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, heteroaryl, cycloalkyl, tetrahydronaphthyl or decahydronaphthyl;R.sup.2 represents hydrogen or methyl; andR.sup.3 and R.sup.4, independently of one another, in each case represent hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, dialkoxyalkyl, hydroxyalkyl, hydroxyalkoxyalkyl, dioxolanylalkyl, oxolanylalkyl, dioxanylalkyl, or in each case optionally substituted cycloalkylalkyl, cycloalkyl, aralkyl, aralkenyl or aryl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bound, represent an optionally substituted saturated heterocyclic ring which may optionally contain further heteroatoms,or acid-addition salts thereof.
    Type: Grant
    Filed: January 25, 1988
    Date of Patent: February 27, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Weissmuller, Dieter Berg, Stefan Dutzmann, Gerd Hanssler
  • Patent number: 4895840
    Abstract: Novel N-(Aryl-,aryloxy-,arylthio-,arylsulfinyl-and arylsulfonyl-)alkyl-N,N'-(or N',N')alkylaminoalkyl ureas, thioureas and cyanoguanidines represented by the following formula: ##STR1## wherein Ar is aryl selected from the group consisting of 1- and 2-naphthyl, 2,3-dihydro-1H-inden-4(or 5)-yl,2-furanylmethyl,2-pyridinyl, phenyl and phenyl substituted by 1-3 radicals commonly used in the pharmaceutical art; (X).sub.d is oxygen, thio, sulfinyl, sulfonyl or d is zero; Z and W are each R or-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 wtih the proviso that when Z is R, W is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2 and when Z is-(CH.sub.2).sub.m -NR.sup.1 R.sup.2, W is R; B is carbonyl, thioxomethyl, or cyanoiminomethyl; R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are selected from the group consisting of hydrogen, loweralkyl, cycloalkyl, phenyl or phenyl-loweralkyl wherein phenyl may be substituted by 1-3 radicals commonly used in the pharmaceutical art; R.sup.1 and R.sup.2, and R.sup.3 and R.sup.
    Type: Grant
    Filed: June 10, 1987
    Date of Patent: January 23, 1990
    Assignee: A. H. Robins Company, Incorporated
    Inventor: James R. Shanklin, Jr.
  • Patent number: 4870074
    Abstract: Compounds of the formula: ##STR1## wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y).sub.p --R.sub.6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R.sub.6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R.sub.1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R.sub.2 is hydrogen; R.sub.3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R.sub.4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R.sub.5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R.sub.2, R.sub.3 and R.
    Type: Grant
    Filed: April 24, 1987
    Date of Patent: September 26, 1989
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Tatsuya Kon, Shiro Kato, Toshiya Morie, Kazunori Ohno, Katsuhiko Hino, Tadahiko Karasawa, Naoyuki Yoshida
  • Patent number: 4837350
    Abstract: Benzoin esters of aromatic sulfonic acids can be obtained in high yield from benzoin and the respective sulfonyl halide in molar amounts of a base by carrying out the reaction at low temperature in an organic solvent with the addition of water. Aqueous NaOh or KOH can be used as base in this process.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: June 6, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Rutsch, Rinaldo Husler
  • Patent number: 4818757
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: December 28, 1987
    Date of Patent: April 4, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4798892
    Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: January 17, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
  • Patent number: 4774334
    Abstract: Compounds possessing antiallergy activity have the formula: ##STR1## wherein R and R.sup.1 are independently hydrogen or alkyl, or R and R.sup.1 together with the attached nitrogen form a heterocyclic ring system selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl and 1, 2, 3, 4-tetrohydroquinolinyl, and R.sup.2 is phenyl or phenyl monosubstituted with a lower alkyl, a nitro, a halogenated methyl, a halogen or a lower alkoxy group.
    Type: Grant
    Filed: November 9, 1987
    Date of Patent: September 27, 1988
    Assignee: Pennwalt Corporation
    Inventors: Vassil S. Georgiev, Thomas R. DeCory
  • Patent number: 4748280
    Abstract: The 2-chloro-1,1,1-tri(C.sub.1 -C.sub.6)alkoxyethanes are prepared from the corresponding tri(C.sub.1 -C.sub.6)alkoxyethanes by chlorination with N-chlorosuccinimide or with chlorine in pyridine and a chlorohydrocarbon cosolvent.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: May 31, 1988
    Assignee: Pfizer Inc.
    Inventors: Banavara L. Mylari, William J. Zembrowski
  • Patent number: 4736055
    Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 5, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
  • Patent number: 4727072
    Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.
    Type: Grant
    Filed: February 12, 1986
    Date of Patent: February 23, 1988
    Assignee: McNeilab, Inc.
    Inventors: Philip P. Grous, Richard J. Mohrbacher
  • Patent number: 4659721
    Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: April 21, 1987
    Assignee: Ludwig Heumann & Co. GmbH
    Inventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
  • Patent number: 4656180
    Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.
    Type: Grant
    Filed: March 5, 1985
    Date of Patent: April 7, 1987
    Assignee: Ludwig Heumann & Co., GmbH
    Inventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
  • Patent number: 4634701
    Abstract: Compounds of formula (I): ##STR1## wherein: A represents a CH-NO.sub.2 group or a N-CN group;B represents CH.sub.2, O, S or a direct bond;R represents a bicyclic or polycyclic residue, variously substituted and functionalized;R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or C.sub.1 -C.sub.4 alkyl groups; andn and m, which may be the same or different, are 0, 1, 2, 3 or 4;are valuable pharmacological agents.
    Type: Grant
    Filed: May 28, 1985
    Date of Patent: January 6, 1987
    Assignee: Ausonia Farmaceutici s.r.l.
    Inventor: Leonardo De Vincentiis
  • Patent number: 4613596
    Abstract: New compounds active in the treatment of ulcers and alergic skin symptoms are prepared by reacting 2-[[5-[(dimethylamino)methyl]furfuryl]thio]ethylmethylsulphide with a suitable compound of formula RH. Said compounds are particularly useful as active principles in pharmaceutical compositions for use in the treatment of affections which require the administration of antagonists for histamine H.sub.2 receptors.
    Type: Grant
    Filed: December 16, 1985
    Date of Patent: September 23, 1986
    Assignee: Magis Farmaceutrici s.r.l.
    Inventor: Adolfo Moroni
  • Patent number: 4595758
    Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.
    Type: Grant
    Filed: December 3, 1984
    Date of Patent: June 17, 1986
    Assignee: Bristol-Myers Company
    Inventors: Ronnie R. Crenshaw, Aldo A. Algieri
  • Patent number: 4588826
    Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.
    Type: Grant
    Filed: December 3, 1984
    Date of Patent: May 13, 1986
    Assignee: Bristol-Myers Company
    Inventors: Ronnie R. Crenshaw, Aldo A. Algieri
  • Patent number: 4585791
    Abstract: The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: April 29, 1986
    Assignee: Farmitalia Carlo Erba, S.p.A.
    Inventors: Franco Faustini, Achille Panzeri, Fabrizio Orzi, Enrico di Salle, Roberto Ceserani
  • Patent number: 4563527
    Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.
    Type: Grant
    Filed: July 19, 1984
    Date of Patent: January 7, 1986
    Assignee: Torii & Co., Ltd.
    Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shin-ichi Watanabe, Toshiyuki Okutome, Yojiro Sakurai, Masateru Kurumi, Takuo Aoyama
  • Patent number: 4556649
    Abstract: Insecticidally active novel substituted malonic acid diamide insecticides of the formula ##STR1## wherein R.sup.1 represents aryl or heteroaryl, each of which can optionally be substituted,R.sup.2 represents hydrogen or trialkylsilyl, and represents alkyl, cycloalkyl, alkenyl, alkinyl, aralkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphenyl, arylsulphenyl, alkylsulphonyl, arylsulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, arylaminosulphonyl or arylalkylaminosulphonyl, each of which can optionally be substituted, and represents radicals of the formula--CO--NR.sup.5 R.sup.6whereinR.sup.5 and R.sup.6 independently of one another represent hydrogen, alkyl, cycloalkyl, aryl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphonyl or arylsulphonyl, it being possible for these radicals to be optionally substituted,R.sup.3 represents hydrogen or the radical R.sup.4,R.sup.7 and R.sup.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: December 3, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
  • Patent number: 4539416
    Abstract: A process for making N-furfurylthioalkyl carboxamide by reacting an oxaz(ol)ine with furfurylmercaptan in the absence of a transition metal catalyst. The carboxamide may then be hydrolyzed to form the 2-furfurylthioalkylamine.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: September 3, 1985
    Assignee: The Dow Chemical Company
    Inventors: Harold G. Fravel, Jr., Michael J. Fazio
  • Patent number: 4537989
    Abstract: A compound of the formula ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) or ##STR4## (R.sup.6 is as defined above), R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.
    Type: Grant
    Filed: April 15, 1983
    Date of Patent: August 27, 1985
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Keiichi Ono, Akihiko Sugie, Masami Muraoka, Michihiro Yamamoto
  • Patent number: 4517366
    Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.
    Type: Grant
    Filed: April 16, 1984
    Date of Patent: May 14, 1985
    Assignee: Bristol-Myers Company
    Inventors: Ronnie R. Crenshaw, Aldo A. Algieri
  • Patent number: 4482549
    Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.
    Type: Grant
    Filed: February 8, 1984
    Date of Patent: November 13, 1984
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
  • Patent number: 4474782
    Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts possess analgesic and/or opiate antagonistic activity. In the formula R.sup.1 represents lower alkyl; R.sup.2 represents hydrogen, lower alkyl or (lower)alkoxymethyl; R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents a lower alkenyl or lower alkynyl group containing at least 3 carbon atoms and in which there is no unsaturated bond in the 1-position.
    Type: Grant
    Filed: February 24, 1984
    Date of Patent: October 2, 1984
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Alan C. White, Edwin T. Edington
  • Patent number: 4470932
    Abstract: Carboxylic acid anhydrides of the general formulaR--CO--O--CO--R' (I)in whichR and R' are identical or different and represent an optionally substituted alkyl group having 1 to 18 carbon atoms, an optionally substituted cycloalkyl group having 3 to 12 carbon atoms or an optionally substituted aryl group, or represent an optionally substituted 5-membered or 6-membered heterocyclic radical which additionally can be fused to a benzene ring,are obtained in high yields by a process in which a trimethylsilyl carboxylate of the general formulaR--CO--OSi(CH.sub.3).sub.3 (II)in whichR has the meaning given above, is reacted with a carboxylic acid-halide of the general formulaR'CO--X (III)in whichR' has the meaning given above, andX represents a halogen atom, if appropriate in the presence of a catalyst and, if appropriate, in the presence of a diluent, at a temperature between 20.degree. and 250.degree. C.The carboxylic acid anhydrides are valuable intermediate products for organic syntheses.
    Type: Grant
    Filed: October 22, 1982
    Date of Patent: September 11, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventor: Kurt Findeisen
  • Patent number: 4459410
    Abstract: Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.
    Type: Grant
    Filed: October 5, 1981
    Date of Patent: July 10, 1984
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
  • Patent number: 4455436
    Abstract: The invention relates to N-acyl-o-phenylenediamines of the formula ##STR1## wherein A is a colorless carbocyclic or heterocyclic aromatic radical and each of R.sub.1 and R.sub.2 independently is an alkyl, alkenyl or phenyl radical which is unsubstituted or substituted by non-chromophoric groups, but only one of R.sub.1 and R.sub.2 can be phenyl, and the ring B can also be substituted by non-chromophoric groups. The invention also relates to processes for the manufacture of these compounds, their use for whitening man-made organic material their conversion into benzimidazolium compounds as well as stable, concentrated aqueous solutions of such compounds, processes for their manufacture and their use for whitening manmade organic material.
    Type: Grant
    Filed: August 14, 1981
    Date of Patent: June 19, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans R. Meyer, Max Siegrist
  • Patent number: 4440781
    Abstract: A method for producing a psychotropic response, especially for alleviating the symptoms of alcohol withdrawal, comprises administering to a human or animal subject in need thereof a psychotropically effective non-toxic amount of an oxyoctadecanoate. A composition for use in the present method is provided.
    Type: Grant
    Filed: June 11, 1982
    Date of Patent: April 3, 1984
    Assignee: The Vinoxen Company, Inc.
    Inventors: Herman P. Benecke, Bob E. Sherwood
  • Patent number: 4438111
    Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans--CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturtaed heterocyclic amino group; andR.sup.4 is thienylalkyl or furanylalkyl in which the ring may be substituted.These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.
    Type: Grant
    Filed: September 17, 1982
    Date of Patent: March 20, 1984
    Assignee: Glaxo Group Limited
    Inventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis