Polycyclo Ring System Patents (Class 514/510)
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4960792Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James
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Patent number: 4959383Abstract: Phenylsulfone alkenoic acids and derivatives thereof are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR wherein R is hydrogen, alkali metal or lower alkyl or X is 5-tetrazolyl or ##STR2## wherein R' is lower alkyl or aryl; n is 2, 3 or 4 and m is 2, 3 or 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic disease.Type: GrantFiled: October 31, 1988Date of Patent: September 25, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Steven E. Hall
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Patent number: 4948582Abstract: Disclosed are pharmaceutical compositions containing naphthoic acid derivatives and method of use for enhancing oxygen availability to mammailian tissue.Type: GrantFiled: May 11, 1989Date of Patent: August 14, 1990Assignee: Rorer Pharmaceutical CorporationInventors: John T. Suh, Robert G. Pendleton, Charles E. Pendley, II, Kin T. Yu, Paul R. Menard, Alain B. Schreiber
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Patent number: 4946864Abstract: Novel HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: February 1, 1988Date of Patent: August 7, 1990Assignee: Merck & Co., Inc.Inventors: John Prugh, Albert A. Deana, Clarence S. Rooney
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Patent number: 4946845Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: November 25, 1988Date of Patent: August 7, 1990Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
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Patent number: 4945108Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.Type: GrantFiled: April 24, 1989Date of Patent: July 31, 1990Assignee: Hoechst AktiengesellschaftInventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
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Patent number: 4939261Abstract: Disclosed are compounds of the formula ##STR1## wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R.sub.0 independently represent hydrogen, lower alkyl, (C.sub.3 -C.sub.7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C.sub.2 -C.sub.5)-alkylene; or A represents straight chain (C.sub.2 -C.sub.Type: GrantFiled: September 17, 1987Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventor: Gary M. Ksander
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Patent number: 4937264Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: June 30, 1989Date of Patent: June 26, 1990Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
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Patent number: 4937263Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: July 17, 1989Date of Patent: June 26, 1990Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Ta J. Lee, Robert L. Smith, Clarence S. Rooney
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Patent number: 4935444Abstract: Esterified ephedrine derivatives with prolonged antiulcer activity and low toxicity, having the following general formula: ##STR1## in which R is: ##STR2## The invention also describes a process for preparing derivatives of formula (I) and compositions containing them as active principle.Type: GrantFiled: October 6, 1988Date of Patent: June 19, 1990Assignee: Etablissement TexcontourInventor: Federico Butelman
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Patent number: 4933367Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.Type: GrantFiled: March 12, 1987Date of Patent: June 12, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
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Patent number: 4933165Abstract: A pharmaceutical composition and method of counteracting HMG-CoA reductase inhibitor-associated myopathy is disclosed. The method comprises the adjunct administration of an effective amount of a HMG-CoA reductase inhibitor and an effective amount of Coenzyme Q.sub.10.Type: GrantFiled: January 18, 1989Date of Patent: June 12, 1990Assignee: Merck & Co., Inc.Inventor: Michael S. Brown
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Patent number: 4929642Abstract: A method of combating agricultural pest comprising applying a pesticidally effective amount of a substituted 1,4-naphthoquinone on agricultural pests and/or their environment, said 1,4-naphthoquinone being of the formula ##STR1## in which n represents the number zero or a number from 1 to 12,R.sup.1 represents hydrogen, t-butylcarbonyl or acetyl andR.sup.2 represents phenyl which is substituted by bromine, fluorine, chlorine, trifluoromethyl, trifluoromethoxy, trifluoromethylsulphenyl, trifluoromethylsulphonyl or trimethylsilyl or cyclohexyl which is substituted by methyl, trifluoromethyl or trimethylsilyl orR.sup.2 represents C.sub.1 -C.sub.8 -alkyl which is substituted by fluorine, chlorine or bromine.Type: GrantFiled: June 29, 1988Date of Patent: May 29, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Lindner, Benedikt Becker, Robert Steffens, Ulrike Wachendorff-Neumann, Wilhelm Brandes, Wilhelm Stendel, Stefan Dutzmann
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Patent number: 4927845Abstract: Anthralin analogues containing a thio-substituent, especially in one or more of the positions 2-, 7- and 10- of the anthralin ring. They may be made by reacting an anthralin derivative (e.g. 10-bromoanthralin) with a thiol or a compound containing a group convertible to a thio-group. Alternatively, a 1,8-dihydroxy anthraquinone containing a thio-substituent may be reduced. Reactive intermediates may be made by introducing one or more nuclear allylic groups into a 1,8-dihydroxy anthraquinone and then converting them into a reactive form, e.g. by epoxidation or halide addition. The intermediate can then reduced to the oxidation state corresponding to anthralin.Additional products having the 10-carbon atom of the anthralin ring as part of a heterocyclic ring, may be made by anthralins containing various substitutes thioalkyl groups as the 10-substituent.The compounds are useful for treatment of psoriasis, and may be formulated in the conventional vehicles for topical application, for example petrolatum.Type: GrantFiled: August 15, 1989Date of Patent: May 22, 1990Assignee: The Victoria University of ManchesterInventor: John M. Bruce
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Patent number: 4916157Abstract: There are described novel acylated naphthylamines of the formula I defined herein ##STR1## which have valuable fungicidal properties. They can be used in practice on their own or in the form of compositions for the protection of cultivated plants against fungus infection.Type: GrantFiled: April 3, 1989Date of Patent: April 10, 1990Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Wolfgang Eckhardt, Walter Kunz, Adolf Hubele
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Patent number: 4916156Abstract: The present invention relates to aromatic derivatives of the formula: ##STR1## in which: n represents an integer between 2 and 10;R.sub.1 and R.sub.2 are identical or different and represent a cycloalkyl containing 3 to 6 carbon atoms or an alkyl containing from 1 to 6 carbon atoms which is unsubstituted or substituted by a phenyl or benzyl group; orR.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, form a heterocycle selected from pyrrolidin-1-yl, piperidino, azepin-1-yl, hexamethyleneimino, 4-methylpiperidino, 4-benzylpiperidino, 4-phenylpiperidino, 1,2,3,4-tetrahydroisoquinol-2-yl, morpholino and imidazol-1-yl groups;R.sub.3 represents a hydrogen, a halogen, a methyl or a phenyl;R.sub.4 represents a hydrogen, a halogen or a methyl; or R.sub.3 and R.sub.4, taken together with the benzene ring to which they are bonded, form a naphth-1-yl or naphth-2-yl group;Y represents a direct bond, a methyleneoxy group, a methylenethio group or a vinylene group; andR.sub.Type: GrantFiled: April 6, 1988Date of Patent: April 10, 1990Assignee: SanofiInventors: Madeleine Mosse, Vincenzo Proietto
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Patent number: 4912134Abstract: Azulene derivatives of the following formula ##STR1## wherein R.sup.1 stands for an alkyl group of 1 to 3 carbon atoms, R.sup.2 stands for an alkyl group of 1 to 3 carbon atoms, and R.sup.3 is at the 5- or 6-position and stands for an alkyl group of 1 to 6 carbon atoms, an aryl group of 6 to 9 carbon atoms or an aralkyl group of 7 to 10 carbon atoms; have antihyperlipidemic activity. Many of the compounds are also novel per se.Type: GrantFiled: March 10, 1988Date of Patent: March 27, 1990Assignee: Ajinomoto Company, Inc.Inventors: Masabumi Yasunami, Kahei Takase, Takashi Meguro, Katsumi Suzuki, Osamu Hiwatashi, Masaru Okutsu, Nobuo Kato, Toru Nakamura
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Patent number: 4910226Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: December 1, 1987Date of Patent: March 20, 1990Assignee: SmithKline Beckman CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4904661Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 16, 1987Date of Patent: February 27, 1990Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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Patent number: 4892864Abstract: Pharmaceutical and cosmetic compositions contain as the active component 10-acetyl-1,8,9-triacetoxy anthracene.Type: GrantFiled: February 8, 1988Date of Patent: January 9, 1990Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Gerard Lang, Jean Maignan
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Patent number: 4876280Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl or t-butyl, R.sub.2 is hydrogen or C.sub.1-3 alkyl,R.sub.3 is hydrogen or C.sub.1-3 alkyl,R.sub.4 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl or t-butyl,R.sub.5 is hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy,R.sub.6 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, fluoro, chloro, trifluoromethyl, phenoxy or benzyloxy, with the provisos that not more than one of R.sub.5 and R.sub.6 is trifluoromethyl, not more than one of R.sub.5 and R.sub.6 is phenoxy, and not more than one of R.sub.5 and R.sub.6 is benzyloxy, orR.sub.5 and R.sub.6 are attached to adjacent carbon atoms and taken together form a radical of the formula --CH.dbd.CH--CH.dbd.CH--,R.sub.6a is hydrogen, C.sub.1-2 alkyl, fluoro or chloro,X is --CH.sub.2 CH.sub.2 -- or ##STR2## wherein R.sub.7 is hydrogen or C.sub.1-3 alkyl, andR.sub.8 is hydrogen, R.Type: GrantFiled: March 10, 1988Date of Patent: October 24, 1989Assignee: Sandoz Pharm. Corp.Inventor: Robert E. Damon, II
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Patent number: 4876279Abstract: Novel 3-hydroxy-3-methylglutaryl-Coenzyme A(HMG-CoA) reductase inhibitors, which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II) ##STR1## and pharmaceutically acceptable salts of the compound (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 26, 1988Date of Patent: October 24, 1989Assignee: Merck & Co., Inc.Inventors: Ta J. Lee, William F. Hoffman, Clarence S. Rooney
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4866093Abstract: The dihydro-M-4 and dihydro-IsoM-4 hydroxy carboxylic acids of the formula (II): ##STR1## wherein one of R.sup.1 represents a hydrogen atom and the other represents a hydroxy group and wherein the structure shown as ##STR2## represents a structure of formula ##STR3## and the salts and esters of said acids. The invention also provides pharmaceutical compositions containing said acids, salts and/or esters which are useful for inhibiting cholesterol biosynthesis in the liver.Type: GrantFiled: March 19, 1984Date of Patent: September 12, 1989Assignee: Sankyo Company LimitedInventors: Akira Terahara, Minoru Tanaka
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Patent number: 4863926Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.Type: GrantFiled: November 10, 1987Date of Patent: September 5, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
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Patent number: 4861795Abstract: Disclosed are pharmaceutical compositions containing naphthoic acid derivatives and method of use for enhancing oxygen availability to mammailian tissue.Type: GrantFiled: June 23, 1988Date of Patent: August 29, 1989Assignee: Rorer Pharmaceutical CorporationInventors: John T. Suh, Robert G. Pendelton, Charles E. Pendley, II, Kin T. Yu, Paul R. Menard, Alain B. Schreiber
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Patent number: 4859701Abstract: Azulene derivatives of the following formula ##STR1## wherein R.sup.1 stands for an alkyl group of 1 to 3 carbon atoms, R.sup.2 stands for an alkyl group of 1 to 3 carbon atoms, and R.sup.3 is at the 5- or 6- position and stands for an alkyl group of 1 to 6 carbon atoms, an aryl group of 6 to 9 carbon atoms or an aralkyl group of 7 to 10 carbon atoms; have antihyperlipidemic activity. Many of the compounds are also novel per se.Type: GrantFiled: November 6, 1987Date of Patent: August 22, 1989Assignee: Ajinomoto Co., Inc.Inventors: Masabumi Yasunami, Kahei Takase, Takashi Meguro, Katsumi Suzuki, Osamu Hiwatashi, Masaru Okutsu, Nobuo Kato, Toru Nakamura
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Patent number: 4853412Abstract: Disclosed herein are N-[[6-methoxy-5-(trifluoromethyl)-1-naphthalenyl][substituted imino]methyl]-N-methylglycines and methods for their preparation. The N-methylglycines are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: December 23, 1987Date of Patent: August 1, 1989Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Kazimir Sestanj
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Patent number: 4840951Abstract: Naphthalene derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted benzene ring; each of R.sup.1 and R.sup.2 is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR2## or either one of R.sup.1 and R.sup.2 is a lower alkoxy group and the other one is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR3## each of R.sup.3 and R.sup.4 is a lower alkoxy group, or one of R.sup.3 and R.sup.4 is a lower alkoxy group and the other is a hydrogen atom; R.sup.5 is a substituted alkyl group, a heterocyclic group, a cycloalkyl group, an alkyl group of at least 5 carbon atoms or alkenyl group; and each of R.sup.6 and R.sup.7 is hydrogen atom or a lower alkyl group and salts thereof are disclosed. Said naphthalene derivative (I) and its salts have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.Type: GrantFiled: June 17, 1987Date of Patent: June 20, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kohki Takashima
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Patent number: 4835179Abstract: Dihydrodibenzocycloheptyliden-ethylene derivatives of the general formula: ##STR1## in which, R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; andR.sub.3 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms or --CO--(C.sub.1 -C.sub.4 alkyl),are disclosed. These compounds are useful in the treatment of ulcer conditions.Type: GrantFiled: May 26, 1987Date of Patent: May 30, 1989Assignee: Sociedad Espanola de Especialidades Farmacotera peuticasInventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
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Patent number: 4835192Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.Type: GrantFiled: February 4, 1988Date of Patent: May 30, 1989Assignee: Pfizer Inc.Inventors: Michael R. Johnson, Lawrence Melvin, Jr.
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Patent number: 4833164Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 19, 1986Date of Patent: May 23, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4820730Abstract: Amidine compounds of formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof are novel and are of use as anti-trypsin, anti-plasmin, anti-kallikrein, anti-thrombin and anti-complement agents which may be administered orally. These amidine compounds can be produced by the reaction between a carboxylic acid compound of formula (II) ##STR2## or a reactive intermediate thereof and 6-amidino-2-naphthol of formula (III) ##STR3## or preferably an acid addition salt thereof.Type: GrantFiled: July 11, 1988Date of Patent: April 11, 1989Assignee: Torii & Co., Ltd.Inventors: Setsurou Fujii, Toshiyuki Okutome, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shinichi Watanabe, Masateru Kurumi, Takuo Aoyama
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Patent number: 4820727Abstract: Disclosed herein are N-acyl-N-naphthoylglycines and methods of their preparation. The N-acyl-N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: December 23, 1987Date of Patent: April 11, 1989Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Kazimir Sestanj
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Patent number: 4803221Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803222Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4797391Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9,9a-disubstituted-2,3,9,9a-tetrahydro-fluoren-7-yl)o xy]alkanoic acids and alkanimidamides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.Type: GrantFiled: February 8, 1988Date of Patent: January 10, 1989Assignee: Merck & Co., Inc.Inventors: Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr., Adolph M. Pietruszkiewicz
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Patent number: 4792556Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.Type: GrantFiled: April 28, 1986Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
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Patent number: 4791123Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: 4791138Abstract: The present invention provides a novel methoda for preventing deep vein thrombosis comprising the administration of lipoxygenase inhibitors of Formula I ##STR1##Type: GrantFiled: June 25, 1986Date of Patent: December 13, 1988Assignee: The Upjohn CompanyInventor: Robert G. Schaub
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Patent number: 4788187Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: February 26, 1988Date of Patent: November 29, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4788218Abstract: Novel compounds having the general formula: ##STR1## wherein: R.sup.1 is hydrogen or an acyl substituent of the formula:--(C.dbd.O)--R.sup.2wherein:R.sup.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkylene, haloalkyl, aryl, haloaryl or arylalkylene are described. These compounds have both gonadotropic and antigonadotropic properties depending upon the dosage level, and are therefore useful in therapy in the control of male fertility in mammals, particularly in human beings. These compounds combine gonadotropic, antigonadotropic and androgenic properties in the same compound. Their use with LHRH antagonists on male fertility control is also disclosed.Type: GrantFiled: April 28, 1986Date of Patent: November 29, 1988Assignee: SRI InternationalInventors: Masato Tanabe, David F. Crowe, George Detre, Peters, Richard H., Mitchell A.g34 Avery
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Patent number: 4786652Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X is the same and is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6,whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.Type: GrantFiled: March 9, 1987Date of Patent: November 22, 1988Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti
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Patent number: 4785018Abstract: A compound of the formula (I): ##STR1## wherein R is hydrogen or unsubstituted or substituted 1-naphthyl. These compounds are useful to obtain inhibition of aldose reductase in animals, including humans.Type: GrantFiled: June 25, 1987Date of Patent: November 15, 1988Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masao Murase, Shigeaki Maruo
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Patent number: 4769389Abstract: New Orginal derivates of D,L-glutamic acid and D,L-aspartic acid are described having the formula: ##STR1## where n is 1 or 2, R.sub.1 is a mono- or di-substituted phenyl group substituted with halogens such as chlorine and fluorine or with a methyl group in the 3 and 4 positions and in which R.sub.2 consists of a linear or branched alkyl group with 4 to 7 carbon atoms (preferably a pentyl group) and R.sub.3 is an alkyl group having 3 to 6 carbon atoms overall and containing an oxygen atom in the form of an either linkage, such as for example the groups 2-ethoxyethyl, 3-methoxypropyl, 3-ethoxypropyl etc. or in the form of a hydroxyl group such as for example 3-hydroxypropyl etc.The compounds have antagonistic activity towards bio-active polypeptides and are usable particularly in the treatment of illnesses of the digestive tract, of the central nervous system and anorexia and of all those affections (for example tumours) in which exogenic or endogenic bio-active polypeptides are involved.Type: GrantFiled: December 17, 1986Date of Patent: September 6, 1988Assignee: Rotta Research Laboratories, S.p.A.Inventors: Francesco Makovec, Rolando Chiste', Lucio Rovati, Luigi Rovati
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Patent number: 4767625Abstract: A lamella type, single phase liquid crystal composition is prepared from a hydrophilic nonionic surfactant, a water-soluble substance having a hydroxyl group in a molecule thereof, an oil substance, and water.Oil-base cosmetic compositions including cleansing compositions, massage creams or drugs for external application are incorporated with the liquid crystal.The compositions are readily washed off simply by water, and exhibit good properties of non-stickiness and long storage stability.Type: GrantFiled: August 14, 1986Date of Patent: August 30, 1988Assignee: Kao CorporationInventors: Yuichiro Mitsuno, Keiko Nomaguchi, Toshiyuki Suzuki
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Patent number: 4764528Abstract: Novel 2,4-pentadienoic acid derivatives are disclosed. As the examples are mentioned 3-(4-carboxy-trans, trans-1,3-butadienyl)-6-exo-(3.alpha.-hydroxy-trans-1-octenyl)-7-endo-hydr oxybicyclo[3.3.0]oct-2-ene, 3-(5-carboxy-trans, trans-2,4-pentadienyl)-6-exo-(3.alpha.-hydroxy-trans-1-octenyl)-7-endo-hyd roxybicyclo[3.3.0]oct-2-ene and the like. These compounds are useful as a platelet aggregation inhibitor, especially as a thrombosis-prophylactic agent.Type: GrantFiled: March 10, 1987Date of Patent: August 16, 1988Assignee: Teruo Kabushiki KaishaInventors: Keiko Chiba, Makoto Takai, Toshio Wakabayashi
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Patent number: 4760061Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: July 26, 1988Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Brian S. Tait
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Patent number: 4758587Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X and Y are different and are either R.sup.4 or --C(O)W whereinR.sup.4 is lower alkyl or optionally substituted phenyl-lower-alkyl;W is --OR.sup.5 or --NR.sup.6 R.sup.7,whereinR.sup.5 is alkyl, optionally substituted phenyl or optionally substituted benzyl; andR.sup.6 and R.sup.7 are independently hydrogen, lower alkyl, cycloalkyl or optionally substituted phenyl.Type: GrantFiled: March 9, 1987Date of Patent: July 19, 1988Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti