Polycyclo Ring System Patents (Class 514/510)
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4960792
    Abstract: 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: Grant
    Filed: May 8, 1989
    Date of Patent: October 2, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James
  • Patent number: 4959383
    Abstract: 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: Grant
    Filed: October 31, 1988
    Date of Patent: September 25, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 4948582
    Abstract: Disclosed are pharmaceutical compositions containing naphthoic acid derivatives and method of use for enhancing oxygen availability to mammailian tissue.
    Type: Grant
    Filed: May 11, 1989
    Date of Patent: August 14, 1990
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John T. Suh, Robert G. Pendleton, Charles E. Pendley, II, Kin T. Yu, Paul R. Menard, Alain B. Schreiber
  • Patent number: 4946864
    Abstract: Novel HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.
    Type: Grant
    Filed: February 1, 1988
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: John Prugh, Albert A. Deana, Clarence S. Rooney
  • Patent number: 4946845
    Abstract: 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: Grant
    Filed: November 25, 1988
    Date of Patent: August 7, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4945108
    Abstract: New angucyclinones with a therapeutic action can be prepared with the aid of a strain of the genus Streptomyces.
    Type: Grant
    Filed: April 24, 1989
    Date of Patent: July 31, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Susanne Grabley, Joachim Wink, Carlo Giani, Gerhard Seibert, Wolfgang Raether, Susanne Dobreff, Axel Zeeck
  • Patent number: 4939261
    Abstract: 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: Grant
    Filed: September 17, 1987
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Gary M. Ksander
  • Patent number: 4937264
    Abstract: 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: Grant
    Filed: June 30, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta J. Lee, Clarence S. Rooney
  • Patent number: 4937263
    Abstract: 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: Grant
    Filed: July 17, 1989
    Date of Patent: June 26, 1990
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta J. Lee, Robert L. Smith, Clarence S. Rooney
  • Patent number: 4935444
    Abstract: 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: Grant
    Filed: October 6, 1988
    Date of Patent: June 19, 1990
    Assignee: Etablissement Texcontour
    Inventor: Federico Butelman
  • Patent number: 4933367
    Abstract: 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: Grant
    Filed: March 12, 1987
    Date of Patent: June 12, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
  • Patent number: 4933165
    Abstract: 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: Grant
    Filed: January 18, 1989
    Date of Patent: June 12, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Michael S. Brown
  • Patent number: 4929642
    Abstract: 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: Grant
    Filed: June 29, 1988
    Date of Patent: May 29, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Lindner, Benedikt Becker, Robert Steffens, Ulrike Wachendorff-Neumann, Wilhelm Brandes, Wilhelm Stendel, Stefan Dutzmann
  • Patent number: 4927845
    Abstract: 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: Grant
    Filed: August 15, 1989
    Date of Patent: May 22, 1990
    Assignee: The Victoria University of Manchester
    Inventor: John M. Bruce
  • Patent number: 4916157
    Abstract: 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: Grant
    Filed: April 3, 1989
    Date of Patent: April 10, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Moser, Wolfgang Eckhardt, Walter Kunz, Adolf Hubele
  • Patent number: 4916156
    Abstract: 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: Grant
    Filed: April 6, 1988
    Date of Patent: April 10, 1990
    Assignee: Sanofi
    Inventors: Madeleine Mosse, Vincenzo Proietto
  • Patent number: 4912134
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: March 27, 1990
    Assignee: Ajinomoto Company, Inc.
    Inventors: Masabumi Yasunami, Kahei Takase, Takashi Meguro, Katsumi Suzuki, Osamu Hiwatashi, Masaru Okutsu, Nobuo Kato, Toru Nakamura
  • Patent number: 4910226
    Abstract: 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: Grant
    Filed: December 1, 1987
    Date of Patent: March 20, 1990
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4904661
    Abstract: 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: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4892864
    Abstract: Pharmaceutical and cosmetic compositions contain as the active component 10-acetyl-1,8,9-triacetoxy anthracene.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: January 9, 1990
    Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)
    Inventors: Braham Shroot, Gerard Lang, Jean Maignan
  • Patent number: 4876280
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: October 24, 1989
    Assignee: Sandoz Pharm. Corp.
    Inventor: Robert E. Damon, II
  • Patent number: 4876279
    Abstract: 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: Grant
    Filed: May 26, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ta J. Lee, William F. Hoffman, Clarence S. Rooney
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4866093
    Abstract: 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: Grant
    Filed: March 19, 1984
    Date of Patent: September 12, 1989
    Assignee: Sankyo Company Limited
    Inventors: Akira Terahara, Minoru Tanaka
  • Patent number: 4863926
    Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: September 5, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
  • Patent number: 4861795
    Abstract: Disclosed are pharmaceutical compositions containing naphthoic acid derivatives and method of use for enhancing oxygen availability to mammailian tissue.
    Type: Grant
    Filed: June 23, 1988
    Date of Patent: August 29, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: John T. Suh, Robert G. Pendelton, Charles E. Pendley, II, Kin T. Yu, Paul R. Menard, Alain B. Schreiber
  • Patent number: 4859701
    Abstract: 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: Grant
    Filed: November 6, 1987
    Date of Patent: August 22, 1989
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masabumi Yasunami, Kahei Takase, Takashi Meguro, Katsumi Suzuki, Osamu Hiwatashi, Masaru Okutsu, Nobuo Kato, Toru Nakamura
  • Patent number: 4853412
    Abstract: 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: Grant
    Filed: December 23, 1987
    Date of Patent: August 1, 1989
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4840951
    Abstract: 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: Grant
    Filed: June 17, 1987
    Date of Patent: June 20, 1989
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Tameo Iwasaki, Kohki Takashima
  • Patent number: 4835179
    Abstract: 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: Grant
    Filed: May 26, 1987
    Date of Patent: May 30, 1989
    Assignee: Sociedad Espanola de Especialidades Farmacotera peuticas
    Inventors: Xavier D. Cirera, Romeo R. Andreoli, Pedro P. Lloveras, Leonida Bruseghini, Jose P. Irurre
  • Patent number: 4835192
    Abstract: 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: Grant
    Filed: February 4, 1988
    Date of Patent: May 30, 1989
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence Melvin, Jr.
  • Patent number: 4833164
    Abstract: 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: Grant
    Filed: March 19, 1986
    Date of Patent: May 23, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Douglas G. Batt
  • Patent number: 4820730
    Abstract: 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: Grant
    Filed: July 11, 1988
    Date of Patent: April 11, 1989
    Assignee: Torii & Co., Ltd.
    Inventors: Setsurou Fujii, Toshiyuki Okutome, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shinichi Watanabe, Masateru Kurumi, Takuo Aoyama
  • Patent number: 4820727
    Abstract: 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: Grant
    Filed: December 23, 1987
    Date of Patent: April 11, 1989
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Kazimir Sestanj
  • Patent number: 4803221
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: February 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4803222
    Abstract: 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: Grant
    Filed: August 28, 1987
    Date of Patent: February 7, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4797391
    Abstract: 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: Grant
    Filed: February 8, 1988
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Otto W. Woltersdorf, Jr., Edward J. Cragoe, Jr., Adolph M. Pietruszkiewicz
  • Patent number: 4792556
    Abstract: 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: Grant
    Filed: April 28, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4791123
    Abstract: 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: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4791138
    Abstract: The present invention provides a novel methoda for preventing deep vein thrombosis comprising the administration of lipoxygenase inhibitors of Formula I ##STR1##
    Type: Grant
    Filed: June 25, 1986
    Date of Patent: December 13, 1988
    Assignee: The Upjohn Company
    Inventor: Robert G. Schaub
  • Patent number: 4788187
    Abstract: 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: Grant
    Filed: February 26, 1988
    Date of Patent: November 29, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
  • Patent number: 4788218
    Abstract: 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: Grant
    Filed: April 28, 1986
    Date of Patent: November 29, 1988
    Assignee: SRI International
    Inventors: Masato Tanabe, David F. Crowe, George Detre, Peters, Richard H., Mitchell A.g34 Avery
  • Patent number: 4786652
    Abstract: 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: Grant
    Filed: March 9, 1987
    Date of Patent: November 22, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti
  • Patent number: 4785018
    Abstract: 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: Grant
    Filed: June 25, 1987
    Date of Patent: November 15, 1988
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masao Murase, Shigeaki Maruo
  • Patent number: 4769389
    Abstract: 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: Grant
    Filed: December 17, 1986
    Date of Patent: September 6, 1988
    Assignee: Rotta Research Laboratories, S.p.A.
    Inventors: Francesco Makovec, Rolando Chiste', Lucio Rovati, Luigi Rovati
  • Patent number: 4767625
    Abstract: 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: Grant
    Filed: August 14, 1986
    Date of Patent: August 30, 1988
    Assignee: Kao Corporation
    Inventors: Yuichiro Mitsuno, Keiko Nomaguchi, Toshiyuki Suzuki
  • Patent number: 4764528
    Abstract: 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: Grant
    Filed: March 10, 1987
    Date of Patent: August 16, 1988
    Assignee: Teruo Kabushiki Kaisha
    Inventors: Keiko Chiba, Makoto Takai, Toshio Wakabayashi
  • Patent number: 4760061
    Abstract: 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: Grant
    Filed: April 24, 1985
    Date of Patent: July 26, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Philip N. Edwards, Brian S. Tait
  • Patent number: 4758587
    Abstract: 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: Grant
    Filed: March 9, 1987
    Date of Patent: July 19, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Michael C. Venuti