Plural Ring Nitrogens In The Additional Hetero Ring Patents (Class 544/270)
  • Patent number: 5719279
    Abstract: Xanthine derivatives of formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkynyl,R.sub.2 is different and is alkyl, alkynyl, phenyl-alkylene, phenyl alkenylene, cycloalkyl, inter alia,R.sub.3 is cycloalkyl, phenyl, norbornane, inter alia andR.sub.4 is hydrogen, methyl, benzyl, inter alia.
    Type: Grant
    Filed: June 11, 1996
    Date of Patent: February 17, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Ulrike Kufner-Muhl, Helmut Ensinger, Joachim Mierau, Franz Josef Kuhn, Erich Lehr, Enzio Muller
  • Patent number: 5714494
    Abstract: Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.
    Type: Grant
    Filed: September 18, 1996
    Date of Patent: February 3, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 5696124
    Abstract: The invention relates to new xanthine derivatives of general formula I, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: December 9, 1997
    Assignee: Boehringer Ingelheim Kg
    Inventors: Ulrike Kufner-Muhl, Karl-Heinz Weber, Gerhard Waither, Werner Stransky, Helmut Ensinger, Gunter Schingnitz, Franz Josef Kuhn, Erich Lehr
  • Patent number: 5532207
    Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 2, 1996
    Assignee: American Cyanamid Company
    Inventors: Barrington Cross, Marinus Los, Robert F. Doehner, Jr., David W. Ladner, Jerry L. Johnson
  • Patent number: 5447933
    Abstract: A novel xanthine derivative of the formula (I): ##STR1## wherein one of R.sup.1 and R.sup.2 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl; and the other represents--(CH.sub.2).sub.m --Xwherein m is 2 or 3, and X is amino substituted phenyl.Q represents ##STR2## (wherein R.sup.3 and R.sup.4 are the same or different and are substituted or unsubstituted alicyclic alkyl), ##STR3## or a pharmacologically accetable salt thereof is disclosed. This derivative has anti-dementia activity.
    Type: Grant
    Filed: November 9, 1992
    Date of Patent: September 5, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Fumio Suzuki, Junichi Shimada, Hiromasa Kato, Akio Ishii, Shizuo Shiozaki
  • Patent number: 5434150
    Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: July 18, 1995
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Volhard Austel, Helmut Pieper, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
  • Patent number: 5409935
    Abstract: The use of xanthine derivatives for the treatment of secondary nerve cell damage and functional disorders after cranio-cerebral traumas (CCT)The use of xanthine derivatives of the formula I ##STR1## and of their physiologically tolerable salts, in which R.sup.1 is oxoalkyl, hydroxyalkyl or alkyl, R.sup.2 is hydrogen or alkyl and R.sup.3 is hydrogen, alkyl, oxoalkyl or an alkyl having up to 6 carbon atoms, whose carbon chain is interrupted by an oxygen atom, for the production of pharmaceuticals for the treatment of disorders which can occur after cranio-cerebral traumas is described.
    Type: Grant
    Filed: July 9, 1992
    Date of Patent: April 25, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Peter Schubert, John J. Grome, Barbara Kittner, Karl Rudolphi, Ulrich Gebert
  • Patent number: 5332744
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: July 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5292740
    Abstract: The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
  • Patent number: 5278165
    Abstract: Oxazolyl derivatives of formula (I) ##STR1## wherein --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- represents a bivalent radical having the formula--CH.dbd.CH--CH.dbd.CH-- (a-1),--N.dbd.CH--CH.dbd.CH-- (a-2),--CH.dbd.N--CH.dbd.CH-- (a-3),--CH.dbd.CH--N.dbd.CH-- (a-4),--CH.dbd.CH--CH.dbd.N-- (a-5),--N.dbd.CH--N.dbd.CH-- (a-6)or--CH.dbd.N--CH.dbd.N-- (a-7);R represents hydrogen or C.sub.1-4 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or hydroxyC.sub.1-6 alkyl; m represents 1 or 2; D represents C.sub.1-4 alkanediyl; B represents NR.sup.2, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.2 is hydrogen or C.sub.1-4 alkyl; n represents 0, 1 or 2; L represents hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula --Alk--R.sup.3 (b-1); --Alk--Y--R.sup.4 (b-2); --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (b-3); or --CH.sub.2 --CHOH--CH.sub.
    Type: Grant
    Filed: March 23, 1993
    Date of Patent: January 11, 1994
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Francois M. Sommen, Ann C. J. Dierckx, Ludwig P. Cooymans
  • Patent number: 5171353
    Abstract: Sulfonamides of the general formula I ##STR1## where R.sup.1 is hydrogen of C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen or substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.4 -alkenyl; C.sub.3 -C.sub.4 -alkynyl or substituted or unsubstituted saturated or singly unsaturated 5- to 7- membered heteroaryl;R.sup.3 and R.sup.4 are halogen; substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxy C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkenylthio, C.sub.2 -C.sub.6 -alkynyl, C.sub.2 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkynylthio, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylthio, C.sub.5 -C.sub.6 -cycloalkenyl, C.sub.3 -C.sub.6 -cycloalkoxy, C.sub.5 -C.sub.6 -cycloalkenyloxy, C.sub.5 -C.sub.6 -cycloalkenylthio, phenyl, phenoxy, phenylthio, benzyl, benzyloxy or benzylthio;the group given for R.sup.2, or NR.sup.7 R.sup.8, where R.sup.7 and R.sup.8 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: December 15, 1992
    Assignee: BASF Akteingesellschaft
    Inventors: Klaus Fischer, Horst Mayer, Klaus Ditrich, Gerhard Hamprecht, Bruno Wuerzer, Karl-Otto Westphalen
  • Patent number: 5158954
    Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: October 27, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 5157026
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: October 20, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 5102880
    Abstract: Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogren atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
    Type: Grant
    Filed: September 5, 1991
    Date of Patent: April 7, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Thomas F. Walsh
  • Patent number: 4879296
    Abstract: The present invention relates to certain novel 8-phenylxanthines substituted in the 3 or 4 position of the phenyl group by an alkenylene, alkenyleneoxy, alkynylene or alkynyleneoxy bearing a terminal acidic grouping, and to their use in human and veterinary therapy, particularly for conditions associated with the cell surface effects of adenosine.
    Type: Grant
    Filed: April 25, 1986
    Date of Patent: November 7, 1989
    Assignee: Burroughs Wellcome co.
    Inventors: Susan M. Daluge, Harry J. Leighton
  • Patent number: 4840949
    Abstract: The invention relates to new oxidiazole-alkyl-purine-derivatives of the Formula I ##STR1## and pharmaceutically acceptable salts thereof wherein A stands for C.sub.1-4 alkylene andR.sup.1 represents C.sub.1-6 alkyl, hydroxyalkyl, halogenoalkyl, carboxyalkyl, C.sub.5-6 cycloalkyl or aminoalkyl of the Formula --(CH.sub.2).sub.n --NR.sup.2 R.sup.3 in which group n is an integer 1-3; R.sup.2 and R.sup.3 each stand for hydrogen or C.sub.1-4 alkyl or together with the adjacent nitrogen atom they are attached to form a 5- or 6-membered nitrogen containing heterocyclic ring which may optionally comprise a further nitrogen atom or an oxygen atom as heteroatom; orR.sup.1 stands for phenyl, hydroxyphenyl, carboxyphenyl, benzyl or dimethoxybenzylThe compounds of the Formula I can be prepared by methods known per se and can be used in therapy as antitussive agents.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: June 20, 1989
    Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.
    Inventors: Dezso Korbonits, Emil Minker, Zoltan Vargai, Gergely Heja, Gabor Kovacs, Agnes Gottsegen, Sandor Antus, Sandor Virag, Andrea Bolehovszky, Jeno Marton, Katalin Marmarosi nee Kellner, Lorand Debreczeni, Laszlo Tardos, Peter Kormoczy, Vera Gergely, Gabor Horvath
  • Patent number: 4737508
    Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: April 12, 1988
    Assignee: Schering Corporation
    Inventors: Raymond G. Lovey, Arthur J. Elliott
  • Patent number: 4684658
    Abstract: The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.
    Type: Grant
    Filed: December 20, 1984
    Date of Patent: August 4, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Louis Fabre, Daniel Farge, Claude James, Daniel Lave
  • Patent number: 4599338
    Abstract: Xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or (C.sub.1 -C.sub.5) alkyl;R.sub.2 is hydrogen, (C.sub.1 -C.sub.5) alkyl optionally having a double bond, or benzyl;R.sub.3 is hydrogen or methyl;A is (CH.sub.2).sub.n, in which n is an integer from 1 to 4, optionally substituted, when n is higher than 1, by hydroxy;X is nitrogen or ##STR2## and the substituents R are each (C.sub.1 -C.sub.5) alkyl or they form together a polymethylene chain from C.sub.4 to C.sub.6, optionally containing an oxygen or a sulfur atom.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of migraine and asthenia.
    Type: Grant
    Filed: January 16, 1985
    Date of Patent: July 8, 1986
    Assignee: Adir, S.A.R.L.
    Inventors: Gilbert Regnier, Claude Guillonneau, Jacques Duhault, Francois Roman
  • Patent number: 4397779
    Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.
    Type: Grant
    Filed: May 28, 1981
    Date of Patent: August 9, 1983
    Assignee: Baxter Travenol Laboratories, Inc.
    Inventors: Ernest V. Groman, Michael D. Cabelli
  • Patent number: 4376767
    Abstract: Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, phenyl, or substituted phenyl having one or more substituents each of which is selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, chloro and dialkylamino wherein the alkyl portions, which can be the same or different, each have 1 to 5 carbon atoms, with the proviso that when R.sub.1 is alkoxy or alkylthio, then R.sub.2 cannot be alkoxy or alkylthio; X and X', which can be the same or different, are each hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.6 alkoxycarbonyl, halo, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 2, 1981
    Date of Patent: March 15, 1983
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth B. Sloan
  • Patent number: 4374835
    Abstract: New compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or sulfur;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB; andR.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy;are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
    Type: Grant
    Filed: January 12, 1981
    Date of Patent: February 22, 1983
    Assignee: Laroche-Navarron, S.A.
    Inventors: Colette Favier, Henri Pinhas, Serge Beranger, Jean-Claude Pascal
  • Patent number: 4297494
    Abstract: Compounds useful as tracers in the radioimmunoassay of xanthine derivatives such as theophylline and pharmacologically related drugs: ##STR1## Wherein at least one R.sub.1, R.sub.3, R.sub.7 or R.sub.8 is a radioiodinated radical and wherein, if not substituted by a radioiodinated radical, the remaining R.sub.1, R.sub.3, R.sub.7 or R.sub.8 groups are otherwise identical to the substituents at these positions in the xanthine derivative to be assayed. Ordinarily, R.sub.1 is hydrogen, acetate or methyl; R.sub.3 is methyl; R.sub.7 is hydrogen, acetate or methyl; and R.sub.8 is hydrogen. The tracers are made by linking radioiodinatable or preradioiodinated radicals to the xanthine derivative which is to be assayed. The tracers may be employed in known radioimmunoassay techniques.
    Type: Grant
    Filed: August 9, 1978
    Date of Patent: October 27, 1981
    Assignee: Baxter Travenol Laboratories, Inc.
    Inventors: Ernest V. Groman, Michael D. Cabelli
  • Patent number: 4275064
    Abstract: Compounds of the formula: ##STR1## useful in treating dermal inflammation in warm-blooded animals are provided.
    Type: Grant
    Filed: April 30, 1979
    Date of Patent: June 23, 1981
    Assignee: INTERx Research Corporation
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan
  • Patent number: 4174442
    Abstract: Compounds which have the general formula ##STR1## and those which can be obtained from them with a Vilsmeier type reagent and have the formula ##STR2## as well as salts thereof, are useful as anti-inflammatory agents.
    Type: Grant
    Filed: February 3, 1978
    Date of Patent: November 13, 1979
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter C. Wade, Thomas P. Kissick
  • Patent number: 4105656
    Abstract: A process for preparing a 3-N-mono-substituted amino-4-substituted-5-pyrazolone which comprises replacing the hydrogen atom of the NH group at the 3-position of a 3-mono-substituted-5-pyrazolone with a protective group, halogenating the resulting compound to introduce a halogen atom into the 4-position, reacting the resulting compound with a 5- or 6-member heterocyclic compound containing two or more nitrogen atoms to replace the halogen atom at the 4-position with a nitrogen containing heterocyclic group, and hydrolyzing the resulting compound to remove the protective group.
    Type: Grant
    Filed: January 31, 1977
    Date of Patent: August 8, 1978
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kotaro Nakamura, Seiji Ichijima, Nobuo Furutachi, Yosio Kosuge