Patents Examined by Donald G. Daus
  • Patent number: 5973160
    Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.
    Type: Grant
    Filed: February 13, 1996
    Date of Patent: October 26, 1999
    Inventors: Michael A. Poss, Jerome L. Moniot, Ivan D. Trifunovich, David J. Kucera, John K. Thottahil, Shu-Hui Chen, Jianmei Wei
  • Patent number: 5972953
    Abstract: The present invention relates to a novel brain cell protective agent having for its active ingredient a morphinan derivative represented with Compound 1 ##STR1## or pharmacologically acceptable acid addition salt thereof. The compounds used in the present invention were found to have excellent defensive effects against brain nerve cell necrosis in both in vitro and in vivo pharmacological evaluations, and can be used as useful preventive and therapeutic agents of ischemic brain disorders, brain nerve cell disorders and dementia.
    Type: Grant
    Filed: November 7, 1996
    Date of Patent: October 26, 1999
    Assignee: Toray Industries, Ltd.
    Inventors: Hiroshi Nagase, Yoshifumi Imamura, Takashi Endo, Susumu Matsuda, Yasushi Miyauchi
  • Patent number: 5968943
    Abstract: Derivatives of camptothecin are disclosed and are represented by the general formula: ##STR1## wherein when R.sub.2 is H, R.sub.1 is a C.sub.2 -C.sub.4 alkyl group, a C.sub.6 -C.sub.15 alkl group, a C.sub.3 -C.sub.8 cycloalkyl group, a C.sub.2 -C.sub.15 alkenyl group or a C.sub.2 -C.sub.15 epoxy group; and when R.sub.2 is a nitro group, R.sub.1 is a C.sub.1 -C.sub.15 alkyl group, a C.sub.2 -C.sub.15 alkenyl group, a C.sub.3 -C.sub.8 cycloalkyl group, or an epoxy group. Processes for mailing these derivatives and for using them in cancer treatment are also disclosed.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: October 19, 1999
    Assignee: The Stehlin Foundation for Cancer Research
    Inventors: Zhisong Cao, Beppino C. Giovanella
  • Patent number: 5968962
    Abstract: A compound of the formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1, S(O).sub.g, or O; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -- aryl, --COR.sub.1--1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1--1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h --aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h --aryl, or halo; R.sub.3 and R.sub.4 are the same or different and are H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy. The compounds are useful antimicrobial agents.
    Type: Grant
    Filed: August 13, 1996
    Date of Patent: October 19, 1999
    Assignee: Pharmacia & Upjohn Company
    Inventors: Richard C. Thomas, Toni-Jo Poel, Michael R. Barbachyn
  • Patent number: 5969147
    Abstract: New pesticidal substituted biphenyloxazolines of the formula (I) in whichA, B, X, m and n have the meanings stated in the description, and new intermediates therefor.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: October 19, 1999
    Assignees: Bayer Aktiengesellschaft, Yashima Chemical Industry Co., Ltd
    Inventors: Reinhard Lantzsch, Albrecht Marhold, Wolfgang Kramer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
  • Patent number: 5965591
    Abstract: An isoxazole compound having the following formula: wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.
    Type: Grant
    Filed: February 26, 1997
    Date of Patent: October 12, 1999
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Junichi Sakai, Yuichi Aizawa, Naozumi Samata, Masao Kozuka, Kenji Yoshimi, Isao Kaneko, Kazuo Koyama
  • Patent number: 5965582
    Abstract: The N-benzylindole- and benzopyrazole derivatives of the general formula 1 ##STR1## possess anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulating effect and are suitable for the preparation of medicaments.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: October 12, 1999
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Guillaume Lebaut, Fabienne Fouchard, Bernhard Kutscher, Peter Emig, Ilona Fleischhauer, Jurgen Schmidt, Stefan Szelenyi
  • Patent number: 5955457
    Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --COCH.sub.2 --S--CH.sub.2 CH.sub.2 --O--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.n --CH.sub.2 --O--CH.sub.2 CH.sub.2 --OCH.sub.3 ; and n=8-450; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    Type: Grant
    Filed: March 23, 1998
    Date of Patent: September 21, 1999
    Assignee: American Home Products Corporation
    Inventors: Hyuk-Koo Lee, Tianmin Zhu
  • Patent number: 5945538
    Abstract: There are provided ammonium oxazole intermediates of formula I and amino oxazolium intermediates of formula II, useful in the manufacture of insecticidal arylpyrrole compounds.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: August 31, 1999
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 5945535
    Abstract: The present invention relates to a new process for preparing norbenzomorphan, the central intermediate step in the preparation of pharmaceutically useful benzomorphan derivatives of general formula 1 ##STR1## especially (-)-(1R,5S,2"R)-3'-hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzomo rphan or ?(-)-(2R,6S,2'R)-3-(2-methoxypropyl)-6,11,11-trimethyl-1,2,3,4,5,6 -hexahydro-2,6-methano-benzo?.alpha.!oxacin-9-ol! (BIII 277).
    Type: Grant
    Filed: May 1, 1998
    Date of Patent: August 31, 1999
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Hanfried Baltes
  • Patent number: 5942522
    Abstract: Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.
    Type: Grant
    Filed: February 26, 1997
    Date of Patent: August 24, 1999
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Jay Weinstein, Margaret Jevnik Gentles
  • Patent number: 5939445
    Abstract: Novel isoxazolidinedione derivatives of the formula (I) ##STR1## wherein R is an optionally substituted aromatic hydrocarbon, an optionally substituted alicyclic hydrocarbon, an optionally substituted heterocyclic group, an optionally substituted condensed heterocyclic group or a group of the formula ##STR2## R.sub.4 is a hydrogen atom, a lower alkyl or a hydroxy; R.sub.5 is a lower alkyl optionally substituted by hydroxy; and P and Q are each a hydrogen atom or P and Q together form a bond, and pharmaceutically acceptable salts thereof. Said novel isoxazolidinedione derivatives and pharmaceutically acceptable salts thereof have superior hypoglycemic and hypolipidemic actions and are useful for the treatment of diabetes and the complications thereof, as well as therapeutic agents for related diseases such as hyperlipidemia.
    Type: Grant
    Filed: January 28, 1998
    Date of Patent: August 17, 1999
    Assignee: Japan Tobacco, Inc.
    Inventor: Hisashi Shinkai
  • Patent number: 5939428
    Abstract: The invention provides a compound of the following formula: ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl; or phenyl;R.sup.2 is hydrogen;an acyl group of the formula --COR.sup.a wherein R.sup.a is C.sub.1-6 alkyl or phenyl; oran acetylalkylcarbonyl group of the formula --CO(CH.sub.2).sub.n COCH.sub.3 wherein n=1-3; andR.sup.3 and R.sup.4 are substituents at different position(s) of the acridine ring (i.e. C-1'-C-8'), and R.sup.3 and R.sup.4 may be the same or different and independently represent:hydrogen;C.sub.1-6 alkyl;C.sub.1-6 alkyloxy;a nitro group;an amino group of the formula --NR.sup.b R.sup.c wherein R.sup.b and R.sup.c may be the same or different and independently represent hydrogen or C.sub.1-6 alkyl;an aminoalkylamino group of the formula --NH(CH.sub.2).sub.n NR.sup.d R.sup.e wherein R.sup.d and R.sup.e may be the same or different and independently represent hydrogen, C.sub.1-6 alkyl, a hydroxyalkyl group of the formula --(CH.sub.2).sub.n OH wherein n=1-3, or C.sub.
    Type: Grant
    Filed: May 4, 1998
    Date of Patent: August 17, 1999
    Assignee: National Health Research Institutes
    Inventors: Tsann-Long Su, Ting-Chao Chou, Felicia Y.-H. Wu, Cheng-Wen Wu
  • Patent number: 5936095
    Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
    Type: Grant
    Filed: June 10, 1997
    Date of Patent: August 10, 1999
    Assignee: Neurogen Corporation
    Inventors: Robert W. DeSimone, Charles A. Blum
  • Patent number: 5935961
    Abstract: Compounds with fungicidal properties having formula I ##STR1## wherein W is CH.sub.3 --O--A.dbd.C(-)--CO(V)CH.sub.3 ;A is N or CH;V is O or NH;R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups and Q is substituted or unsubstituted aryl groups.
    Type: Grant
    Filed: March 30, 1998
    Date of Patent: August 10, 1999
    Assignee: Rohm and Haas Company
    Inventors: Ronald Ross, Steven Howard Shaber
  • Patent number: 5932727
    Abstract: The present invention relates to a process for the preparation of dioxazine derivatives of the formula I ##STR1## in which R.sup.1 is hydrogen or (C.sub.1 -C.sub.8)-alkyl, by ring closure of a compound of the formula II ##STR2## in the presence of a ring-closure agent, wherein the ring-closure agent used is an N-hetarene N-oxide. The compounds of the formula I are used for producing valuable dyes and pigments.
    Type: Grant
    Filed: October 16, 1997
    Date of Patent: August 3, 1999
    Assignee: Clariant GmbH
    Inventors: Gert Nagl, Wolfgang Bauer, Manfred Urban, Dieter Schnaitmann
  • Patent number: 5932588
    Abstract: Camptothecin compounds having a --CH.sub.2 --L group are effective anti-tumor compounds. These compounds inhibit the enzyme topoisomerase I and DNA of associated topoisomerase I-DNA complexes.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: August 3, 1999
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani
  • Patent number: 5932601
    Abstract: 2,4-Oxazolidinedione derivative represented by the formula: ##STR1## wherein R stands for an optionally substituted hydrocarbon residue or heterocyclic group; Y stands for a group represented by --CO--, --CH(OH)-- or --NR.sup.3 -- (wherein R.sup.3 stands for an optionally substituted alkyl group); m is 0 or 1; n is 0, 1 or 2; A stands for a C.sub.1-7 divalent aliphatic hydrocarbon group; R.sup.1 stands for hydrogen or an alkyl group; ring E stands for a benzene ring having 1 or 2 substituents; L and M respectively stand for hydrogen, or L and M may optionally be combined with each other to form a bond; with a proviso that the partial formula: ##STR2## does not include the formula: ##STR3## wherein R' stands for an alkyl group; or a salt thereof, which has excellent actions of lowering blood sugar and lipid in blood.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: August 3, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Hiroyuki Odaka, Yu Momose, Mitsuru Kawada
  • Patent number: 5925773
    Abstract: There are provided ammonium oxazole intermediates of formula I and amino oxazolium intermediates of formula II, useful in the manufacture of insecticidal arylpyrrole compounds.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: July 20, 1999
    Assignee: American Cyanamid Company
    Inventor: Venkataraman Kameswaran
  • Patent number: 5925659
    Abstract: A compound represented by formula I: ##STR1## is disclosed. The compounds are active primarily against gram negative organisms. Pharmaceutical compositions and methods of treatment are also disclosed.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: July 20, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, Ravi Nargund, Meng-Hsin Chen, H. Russell Onishi