Patents Examined by P. G. Spivack
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Patent number: 5504068Abstract: 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: GrantFiled: February 23, 1993Date of Patent: April 2, 1996Assignee: LTT Institute Co., Ltd.Inventors: Katsuo Komiya, Rie Igarashi, Mitsuko Takenaga, Akira Yanagawa, Yutaka Mizushima, Tateo Nishimura, Toshitaka Kudo, Kunio Ando
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Patent number: 5354731Abstract: 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: GrantFiled: February 11, 1992Date of Patent: October 11, 1994Assignee: Nissan Chemical Industries Ltd.Inventors: Kenzi Makino, Katsushi Morimoto, Shigeaki Akiyama, Hideaki Suzuki, Takeshi Nagaoka, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe
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Patent number: 5266711Abstract: 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: GrantFiled: October 16, 1990Date of Patent: November 30, 1993Assignee: SanofiInventors: Bernard Boudet, Jean R. Dormoy, Alain Heymes
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Patent number: 5219868Abstract: 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: GrantFiled: December 4, 1991Date of Patent: June 15, 1993Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Kenji Kodaka, Katsutoshi Kinoshita, Michihiko Nakaya, Koichi Ebihara, Shirou Shiraishi, Eiichi Yamada, Satoshi Numata
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Patent number: 5216162Abstract: 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: GrantFiled: August 28, 1992Date of Patent: June 1, 1993Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Robert M. Kearney
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Patent number: 5210203Abstract: 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: GrantFiled: May 7, 1992Date of Patent: May 11, 1993Assignee: Siska Diagnostics, Inc.Inventors: Gary F. Musso, Soumitra Ghosh, Emil T. Kaiser
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Patent number: 5204476Abstract: 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: GrantFiled: December 18, 1990Date of Patent: April 20, 1993Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Andreas Wachtler, Eike Poetsch, Thomas Geelhaar, Reinhard Hittich, Volker Reiffenrath, Hans-Michael Kompter
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Patent number: 5196538Abstract: 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: GrantFiled: July 18, 1991Date of Patent: March 23, 1993Assignee: Eastman Kodak CompanyInventors: John W. Wilson, Alexandra D. Bermel
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Patent number: 5196539Abstract: 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: GrantFiled: July 18, 1991Date of Patent: March 23, 1993Assignee: Eastman Kodak CompanyInventors: John W. Wilson, Alexandra D. Bermel
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Patent number: 5192779Abstract: 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: GrantFiled: August 28, 1991Date of Patent: March 9, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5190951Abstract: 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: GrantFiled: October 9, 1991Date of Patent: March 2, 1993Assignee: SS Pharmaceutical Co., Ltd.Inventors: Hiroshi Hasegawa, Kazuo Isomae, Takeshi Kotsugai, Noriaki Shioiri, Kumiko Sekine, Naokata Taido, Susumu Sato, Tadayuki Kuraishi
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Patent number: 5185348Abstract: 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: GrantFiled: May 21, 1992Date of Patent: February 9, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5182400Abstract: Process for the preparation of 5-alkylpyridine-2,3-dicarboxylic esters by reaction of 2-oxosuccinic esters with 2-alkylacrolein oximes.Type: GrantFiled: August 7, 1991Date of Patent: January 26, 1993Assignee: Hoechst AktiengesellschaftInventors: Jurgen Weber, Peter Lappe, Helmut Springer
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Patent number: 5182288Abstract: 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: GrantFiled: November 13, 1991Date of Patent: January 26, 1993Assignee: Ortho Pharmaceutical CorporationInventors: William V. Murray, Michael P. Wachter
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Patent number: 5180831Abstract: 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: GrantFiled: August 10, 1990Date of Patent: January 19, 1993Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
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Patent number: 5179100Abstract: 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: GrantFiled: March 9, 1992Date of Patent: January 12, 1993Assignee: Hoechst-Roussel Pharmaceuticals inc.Inventors: Gregory M. Shutske, John D. Tomer, IV
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Patent number: 5177244Abstract: This invention provides a process and intermediates for preparing 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids.Type: GrantFiled: May 7, 1992Date of Patent: January 5, 1993Assignee: Eli Lilly and CompanyInventor: Christopher R. Schmid
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Patent number: 5164508Abstract: 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: GrantFiled: August 28, 1991Date of Patent: November 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans-Joachim Diehr
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Patent number: 5155121Abstract: 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: GrantFiled: August 2, 1991Date of Patent: October 13, 1992Assignee: Bayer AktiengesellschaftInventors: Ulrich Niewohner, Ulrich E. Muller, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Patent number: 5142069Abstract: This invention provides a process and intermediates for preparing 2,2-dimethyl-2,3-dihydrobenzofuran-7-carboxylic acids.Type: GrantFiled: March 7, 1991Date of Patent: August 25, 1992Assignee: Eli Lilly and CompanyInventor: Christopher R. Schmid