Patents Examined by P. G. Spivack
  • Patent number: 5504068
    Abstract: A topical preparation containing cyclosporin as an active ingredient, is disclosed that contains (a) cyclosporin; (b) an organic solvent for dissolving the cyclosporin; (c) an ester of a fatty acid with a monovalent alcohol having a total number of carbon atoms of 8 or more and/or an alkanol amine, each being in liquid state at 25.degree.C; (d) an oily substance in solid state at 25.degree.C; and (e) a surfactant. The cyclosporin is present in a concentration ranging from appoximately 0.1% to 10% by weight and the ester and/or alkanol amine are/is present in a concentration ranging from approximately 1% to 15% by weight. The topical preparations are active against atopic dermatitis, psoriasis and allergic contact dermatitis.
    Type: Grant
    Filed: February 23, 1993
    Date of Patent: April 2, 1996
    Assignee: LTT Institute Co., Ltd.
    Inventors: Katsuo Komiya, Rie Igarashi, Mitsuko Takenaga, Akira Yanagawa, Yutaka Mizushima, Tateo Nishimura, Toshitaka Kudo, Kunio Ando
  • Patent number: 5354731
    Abstract: A pyridinesulfonamide derivative of the formula (I) and a salt thereof: ##STR1## wherein R.sup.1 is a halogen atom, a trifluoromethyl group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a C.sub.1 -C.sub.6 mono- or di-alkylaminocarbonyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 alkylsulfonyl group, a C.sub.1 -C.sub.6 alkylthio group, a C.sub.1 -C.sub.6 alkyl group substituted by a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 alkyl group substituted by a C.sub.1 -C.sub.6 mono- or poly-halogenoalkoxy group, a C.sub.1 -C.sub.6 mono- or poly-halogenoalkoxy group, a C.sub.1 -C.sub.6 mono- or di-alkylaminosulfonyl group, a C.sub.1 -C.sub.6 alkoxyaminosulfonyl group substituted by a C.sub.1 -C.sub.6 alkyl group, a nitro group, a C.sub.1 -C.sub.6 alkyl group substituted by a C.sub.1 -C.sub.6 alkylthio group, a C.sub.1 -C.sub.6 alkyl group substituted by a C.sub.1 -C.sub.6 alkylsulfonyl group, or a C.sub.1 -C.sub.6 alkyl group substituted by a C.sub.1 -C.sub.6 alkoxycarbonyl group;R.sup.
    Type: Grant
    Filed: February 11, 1992
    Date of Patent: October 11, 1994
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Kenzi Makino, Katsushi Morimoto, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe
  • Patent number: 5266711
    Abstract: The invention relates to a process for the preparation of 3-benzoyl benzofuran derivatives of general formula: ##STR1## wherein a benzofuran derivative of general formula: ##STR2## is reacted in situ in the presence of aluminium chloride successively with phosgene or oxalyl chloride, and then with a phenolic derivative of general formula: ##STR3## to produce a complex which is hydrolysed to form the desired compound of 3-benzoyl benzofuran.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: November 30, 1993
    Assignee: Sanofi
    Inventors: Bernard Boudet, Jean R. Dormoy, Alain Heymes
  • Patent number: 5219868
    Abstract: Herein disclosed are novel imidazolidine derivatives of the formula (I) and intermediates of the formula (II) ##STR1## wherein each R represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, a halogen atom, an alkoxy group having from 1 to 6 carbon atoms, a methylenedioxy group, an alkylthio group having from 1 to 4 carbon atoms, a haloalkyl group having from 1 to 2 carbon atoms, a haloalkoxy group having from 1 to 4 carbon atoms, an alkylcarbonyl group having from 1 to 6 carbon atoms, an alkoxycarbonyl.group having from 1 to 6 carbon atoms, a hydroxy group, a cyano group, a nitro group, an alkylamino group having from 1 to 8 carbon atoms, a phenyl group, a phenoxy group, a benzyl group or a halopyridylmethyloxy group, and n is an integer of from 1 to 3, ##STR2## wherein R and n have, respectively, the same meanings as defined above. Processes for preparing the compounds of the formulas (I) and (II) are also described.
    Type: Grant
    Filed: December 4, 1991
    Date of Patent: June 15, 1993
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Kenji Kodaka, Katsutoshi Kinoshita, Michihiko Nakaya, Koichi Ebihara, Shirou Shiraishi, Eiichi Yamada, Satoshi Numata
  • Patent number: 5216162
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is R.sup.1, ##STR2## --SO.sub.2 R.sup.1 or --SO.sub.2 R.sup.3 ; R is hydrogen or lower alkyl;R.sup.1 is unsubstituted or substituted pyridyl, indolyl or quinolinyl; or substituted phenyl, thienyl, furyl, benzothienyl or benzofuryl, where the foregoing substituted moieties are substituted with halo, lower alkylcarbonyl, benzoyl, carboxy, lower alkoxycarbonyl, CON(R).sub.2, SO.sub.2 R.sup.3, cyano or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl, phenyl, halo, lower alkoxy, hydroxy or trifluoromethyl;R.sup.3 is lower alkyl or phenyl;Z is --O--, --NNHR.sup.4, --NNHR.sup.1, --NOR.sup.4, --NOR.sup.1, --NOCH.sub.2 R.sup.1, ##STR3## Y is O or S; R.sup.4 is hydrogen, lower alkyl or phenyl;which by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.
    Type: Grant
    Filed: August 28, 1992
    Date of Patent: June 1, 1993
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Robert M. Kearney
  • Patent number: 5210203
    Abstract: Nucleic acid hybridization probes are provided which comprise an N.sup.4 -(substituted amino)cytosine moiety, wherein the substituted amino group comprises a tag moiety, whereby the probe is detected. Methods of preparing probes of the invention, intermediates used in such methods, and methods of using the probes of the invention in hybridization assays are also provided. Typical tag moieties employed with the probes of the invention are biotinyl, aminothiadiazole and fluorescein derivatives, connected to N.sup.4 -amino groups of modified cytosines of the probe through linker moieties. Probes tagged with biotin are typically detected by binding to the biotinyl moieties, through a streptavidin or avidin molecule, a reporter group which includes streptavidin or avidin and then detecting a signal due to the reporter group.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: May 11, 1993
    Assignee: Siska Diagnostics, Inc.
    Inventors: Gary F. Musso, Soumitra Ghosh, Emil T. Kaiser
  • Patent number: 5204476
    Abstract: The invention relates to fluorophenylpyridines of the formula I: ##STR1## where R.sup.1 and R.sup.2 are substituted and unsubstituted monovalent organic radicals.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: April 20, 1993
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Andreas Wachtler, Eike Poetsch, Thomas Geelhaar, Reinhard Hittich, Volker Reiffenrath, Hans-Michael Kompter
  • Patent number: 5196539
    Abstract: New ester-containing quaternary pyridinium salts are provided having advantageous utility as charge control agents in electrostatographic toners and developers. The salts have the structure: ##STR1## wherein R.sub.1 is alkyl or aryl, X is --CH.sub.2 --.sub.n, Y is hydrogen, alkyl, alkoxy or halogen, Z.sup..crclbar. is an anion and n is an integer from 2 to 6.Such ester-containing quaternary pyridinium salts also cause toner particles containing them to display lower fusing temperature and improved paper adhesion indexes.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: March 23, 1993
    Assignee: Eastman Kodak Company
    Inventors: John W. Wilson, Alexandra D. Bermel
  • Patent number: 5196538
    Abstract: New ester-containing quaternary pyridinium salts are provided having advantageous utility as charge control agents in electrostatographic toners and developers. The salts have the structure: ##STR1## wherein R.sub.1 is alkyl or aryl, X is --CH.sub.2 --.sub.n, Y is hydrogen, alkyl, alkoxy or halogen, Z.crclbar. is an anion and n is an integer from 1 to 6.Such ester-containing quaternary pyridinium salts also cause toner particles containing them to display lower fusing temperatures and improved paper adhesion indexes.
    Type: Grant
    Filed: July 18, 1991
    Date of Patent: March 23, 1993
    Assignee: Eastman Kodak Company
    Inventors: John W. Wilson, Alexandra D. Bermel
  • Patent number: 5192779
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s)R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through an oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.
    Type: Grant
    Filed: August 28, 1991
    Date of Patent: March 9, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
  • Patent number: 5190951
    Abstract: Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.
    Type: Grant
    Filed: October 9, 1991
    Date of Patent: March 2, 1993
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Hasegawa, Kazuo Isomae, Takeshi Kotsugai, Noriaki Shioiri, Kumiko Sekine, Naokata Taido, Susumu Sato, Tadayuki Kuraishi
  • Patent number: 5185348
    Abstract: The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reacton of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkencarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.
    Type: Grant
    Filed: May 21, 1992
    Date of Patent: February 9, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5182400
    Abstract: Process for the preparation of 5-alkylpyridine-2,3-dicarboxylic esters by reaction of 2-oxosuccinic esters with 2-alkylacrolein oximes.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: January 26, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jurgen Weber, Peter Lappe, Helmut Springer
  • Patent number: 5182288
    Abstract: This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.
    Type: Grant
    Filed: November 13, 1991
    Date of Patent: January 26, 1993
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: William V. Murray, Michael P. Wachter
  • Patent number: 5180831
    Abstract: Quaternary pyridinium compounds, their use in inhibiting acetylcholinesterase, their roles in the prophylaxis and treatment of organophosphate poisoning, their roles in anticholinesterase therapy and their roles as agents mimicking or opposing the actions of the natural neurotransmitter acetylcholine.
    Type: Grant
    Filed: August 10, 1990
    Date of Patent: January 19, 1993
    Assignee: Georgia Tech Research Corporation
    Inventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
  • Patent number: 5179100
    Abstract: There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which compounds are useful as analgesic agents.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: January 12, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals inc.
    Inventors: Gregory M. Shutske, John D. Tomer, IV
  • Patent number: 5177244
    Abstract: This invention provides a process and intermediates for preparing 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: January 5, 1993
    Assignee: Eli Lilly and Company
    Inventor: Christopher R. Schmid
  • Patent number: 5164508
    Abstract: The present invention relates to a new process for the preparation of N-(2-chloro-pyridin-5-yl-methyl)-ethylene-diamine of the formula (I) ##STR1## in a technically simple manner in high yield and in very good quality. The new process is characterized in that N-(2-chloro-pyridin-5-yl-methyl)-aminoacetonitrile of the formula (II) ##STR2## is reacted with hydrogen in the presence of ammonia and in the presence of a catalyst and also in the presence of a diluent, at temperatures between 0.degree. C. and 100.degree. C. and a pressure between 1 bar and 100 bar.N-(2-Chloro-pyridin-5-yl-methyl)-ethylenediamine (I) can be used as an intermediate for the preparation of insecticides.
    Type: Grant
    Filed: August 28, 1991
    Date of Patent: November 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans-Joachim Diehr
  • Patent number: 5155121
    Abstract: The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reaction of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkenecarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.
    Type: Grant
    Filed: August 2, 1991
    Date of Patent: October 13, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5142069
    Abstract: This invention provides a process and intermediates for preparing 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: August 25, 1992
    Assignee: Eli Lilly and Company
    Inventor: Christopher R. Schmid