Patents Examined by Philip I. Datlow
  • Patent number: 5482936
    Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 9, 1996
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Kyle J. Lindstrom
  • Patent number: 5480882
    Abstract: Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: January 2, 1996
    Assignee: Italfarmaco S.p.A.
    Inventors: Alberto Sala, Roberto Barani, Francesca Benedini, Giorgio Bertolini, Giancarlo Dona, Gianni Gromo, Silvio Levi
  • Patent number: 5478936
    Abstract: An asymmetric dioxazine compound represented by the following formula (I) in the free acid form: ##STR1## wherein A.sub.1 and A.sub.2 independently of one another are each sulfo, halo, alkyl or alkoxy, W is an unsubstituted or substituted aliphatic or aromatic bridging group, X.sub.1 and X.sub.2 independently of one another are each hydrogen, halo, alkyl, alkoxy or phenoxy, R.sub.1 and R.sub.2 independently of one another are each hydrogen or unsubstituted or substituted alkyl, R.sub.3 and R.sub.4 independently of one another are each hydrogen, halo, alkyl, alkoxy or unsubstituted or substituted amino, Z is a fiber-reactive group, m and n independently of one another are each 0 or 1, provided that m.noteq.n, and l is 1 or 2.
    Type: Grant
    Filed: March 21, 1994
    Date of Patent: December 26, 1995
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kazufumi Yokogawa, Miyao Takahashi, Takahiko Fuzisaki, Yutaka Kayane, Shigeru Kawabata, Naoki Harada
  • Patent number: 5478834
    Abstract: Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active ingredient.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: December 26, 1995
    Assignee: Sanwa Shoyaku Kabushiki Kaisha
    Inventors: Mitsuo Murayama, Takao Mori
  • Patent number: 5478833
    Abstract: Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active ingredient.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: December 26, 1995
    Assignee: Sanwa Shoyaku Kabushiki Kaisha
    Inventors: Mitsuo Murayama, Takao Mori
  • Patent number: 5476848
    Abstract: An optically active compound of formula (I): ##STR1## in which R.sup.3 represents groups of formula --A--COOR.sup.4, whereinA represents alkylene groups having 3 or 5 carbon atoms andR.sup.4 represents hydrogen or an alkyl group having 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: December 19, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Yoshio Iizuka, Takeshi Yamaguchi
  • Patent number: 5475105
    Abstract: Abstract of the Disclosure: Compounds of the formula I ##STR1## where R.sup.1, R.sup.2, n , R.sup.3, A, X, Y and Z have the meanings stated in the description, and the preparation thereof are described. The novel compounds are suitable for controlling diseases , i.e., as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: December 12, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Gerd Steiner, Liiane Unger, Berthold Behl, Hans-Juergen Teschendorf, Rainer Munschauer
  • Patent number: 5472982
    Abstract: An emulsified composition for treating the skin containing diclofenac sodium, a fatty acid and a dialkyl carboxylate, as essential components.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: December 5, 1995
    Assignee: Shiseido Company Ltd.
    Inventor: Takashi Suzuki
  • Patent number: 5472968
    Abstract: Compounds of formula (I), ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, C.sub.1-6 alkyl, R.sub.3 and R.sub.4 independently represent one or more radicals selected from hydrogen, OH, NH.sub.2, NO.sub.2, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkoxy and n is an integer from 1-2 inclusive, and pharmaceutically acceptable derivatives thereof are useful as pharmaceuticals; in particular, they possess N-methyl-(d)-aspartate(NMDA) blocking properties and are useful in the treatment and/or prevention of neurodegenerative conditions.
    Type: Grant
    Filed: March 16, 1993
    Date of Patent: December 5, 1995
    Assignee: Fisons Corporation
    Inventors: Ronald C. Griffith, James R. Matz, James J. Napier
  • Patent number: 5470850
    Abstract: 2,3,4,5-Tetrahydro-1H-3-benzazepines having the general formula ##STR1## wherein R.sup.1 is Cl or Br; R.sup.3 and R.sup.4 are hydrogen, halogen, CF.sup.3, CN, NO.sub.2, or NH.sub.2.The compounds are useful in treatment of certain disorders in the central nervous system.
    Type: Grant
    Filed: May 6, 1994
    Date of Patent: November 28, 1995
    Assignee: Novo Nordisk A/S
    Inventors: Christian Foged, Rolf Holweg, Erik Nielsen
  • Patent number: 5470880
    Abstract: A method for visibly reducing a skin wrinkle by topically applying to the wrinkle citric acid or a topically salt thereof.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: November 28, 1995
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5470851
    Abstract: Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) ##STR1##
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: November 28, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Takeshi Yamaguchi, Takeshi Oshima, Fumitoshi Asai, Yasuteru Iijima
  • Patent number: 5468743
    Abstract: The present invention is concerned with novel imidazo[2, 1-b][3]benzazepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.4 represents hydrogen, C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, phenyl or halo; R.sup.5 represents hydrogen, C.sub.1-4 alkyl or halo; L represents hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted with one substituent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: November 21, 1995
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Gaston S. M. Diels, Joseph E. Leenaerts
  • Patent number: 5468858
    Abstract: 3,7-Diazabicyclo[3.3.1]nonanes and selected derivatives thereof of the general formula: ##STR1## are disclosed as multiclass antiarrhythmic agents.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: November 21, 1995
    Assignee: The Board of Regents of Oklahoma State University Physical Sciences
    Inventors: Kenneth D. Berlin, Gregory L. Garrison, Subbiah Sangiah, Cyril R. Clarke, Chun-Lin Chen, Ralph Lazzara, Benjamin J. Scherlag, Eugene S. Patterson, George E. Burrows
  • Patent number: 5468854
    Abstract: Conjugates of fluorescent labels with specific, selective, and high affinity ligands for receptors have been synthesized and used to directly measure binding to receptors. In the examples, fluorescein conjugates of the high-affinity benzodiazepine receptor ligands Ro 15-1788 and Ro 7-1986 were synthesized. The binding of these fluorescent ligands (BD 621, BD 623 and BD 607) to benzodiazepine receptors was characterized by direct fluorescence measurement. Both the equilibrium dissociation constants (K.sub.D) of BD 621 and BD 607 and the maximum number of binding sites (B.sub.max) estimated by fluorescence monitoring were consistent with values obtained by using radioligand binding techniques. The binding of BD 621 and BD 607 assessed by fluorescence measurement was reversible, abolished by photoaffinity labeling with Ro 15-4513, and unaffected by a variety of substances that do not bind to benzodiazepine receptors.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: November 21, 1995
    Assignee: Pharmaceutical Discovery Corporation
    Inventors: R. Tyler McCabe, Brian R. de Costa
  • Patent number: 5468740
    Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: November 21, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Shuhei Miyazawa, Richard S. J. Clark, Shinya Abe, Tetsuya Kawahara, Naoyuki Shimomura, Osamu Asano, Hiroyuki Yoshimura, Mitsuaki Miyamoto, Yoshimori Sakuma, Kenzo Muramoto, Hiroshi Obaishi, Koukichi Harada, Hajime Tsunoda, Satoshi Katayama, Kouji Yamada, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5466683
    Abstract: The present invention relates to novel water-soluble analogs of carbamazepine and compositions containing them. The novel compositions are particularly suited for intravenous administration. The analogs of carbamazepine are useful in the treatment of epilepsy and related disorders.
    Type: Grant
    Filed: August 25, 1994
    Date of Patent: November 14, 1995
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Jeff Sterling, Yaacov Herzig
  • Patent number: 5462725
    Abstract: 2-Pyridylmethylenepolyazamacrocyclophosphonic acid compounds and their derivatives are disclosed which may form inert complexes with Gd, Mn or Fe ions. The overall charge of the complex can be varied to alter the in vivo biolocalization. The complexes are useful as contrast agents for diagnostic purposes.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: October 31, 1995
    Assignee: The Dow Chemical Company
    Inventors: Garry E. Kiefer, Won D. Kim
  • Patent number: 5463051
    Abstract: Disclosed are a process and intermediates of the formulae ##STR1## wherein X.sup.- is halide, BF.sub.4.sup.-, R.sup.3 SO.sub.3.sup.-, wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.
    Type: Grant
    Filed: September 27, 1993
    Date of Patent: October 31, 1995
    Assignee: Schering Corporation
    Inventors: Donald Hou, Richard W. Draper, Gary M. Lee, Janet L. Mas, Ingrid Mergelsberg
  • Patent number: 5462936
    Abstract: A compound of the formula: ##STR1## wherein X is .dbd.N--A--R.sup.1 or .dbd.C(R.sup.1)R.sup.2 ; A is a single bond, polymethylerie or --CO--; R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, unsubstituted or substituted phenyl, optionally substituted benzhydryl, or optionally substituted 5 to 6 membered heterocyclic group; Y is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-6 alkoxy, optionally substituted phenoxy, optionally substituted benzyloxy, or optionally substituted benzyl; Z is hydrogen or acyl; n is an integer of from 2 to 6, and pharmaceutically acceptable salt thereof. A pharmaceutical composition containing the compound, which is useful for treating hypertension and cardiac diseases, is also provided.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: October 31, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Teruo Yamamori, Hiroshi Harada, Katsunori Sakai, Kazumi Iwaki, Kazuki Matsunaga