Polycyclo Ring System Patents (Class 562/427)
  • Patent number: 5298511
    Abstract: The invention concerns alkanoic acid derivatives of the formula I ##STR1## wherein Ar.sup.1 is optionally-substituted phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3 C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;n is 0, 1 or 2 and R.sup.1 is halogeno, (1-4 C)alkyl, (1-4 C)alkoxy or fluoro-(1-4 C)alkyl;each of R.sup.2 and R.sup.3 is (1-4 C)alkyl, (2-4 C)alkenyl or (2-4 C)alkynyl; andR.sup.4 is hydrogen or (1-4 C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
    Type: Grant
    Filed: September 23, 1992
    Date of Patent: March 29, 1994
    Assignees: Imperial Chemical Industries PLC, I.C.I. Pharma
    Inventor: David Waterson
  • Patent number: 5294598
    Abstract: This invention relates to 3-substitutedbenzoyl-bicyclo[4,4,0]heptane-2,4-dione with high herbicidal activity represented by formula I ##STR1## wherein one of R.sub.1 or R.sub.2 represents methyl and the other represents hydrogen or lower alkyl or alkoxycarbonyl or its salt.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: March 15, 1994
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Hiroyuki Adachi, Katsunori Tanaka, Takashi Kawana, Hideo Hosaka
  • Patent number: 5252601
    Abstract: The present invention relates to novel 2-mercaptomethylene-tetrahydronaphthalene derivatives which are useful as enkephalinase inhibitors.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: October 12, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight
  • Patent number: 5246965
    Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: September 21, 1993
    Assignee: Ciba-Geigy
    Inventor: Alan J. Main
  • Patent number: 5225595
    Abstract: Sulfonyl compounds of the formula ##STR1## where Ar is the radical of a benzene or naphthalene ring,R.sup.1 and R.sup.2 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -alkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, cyano, halogen or hydroxysulfonyl,R.sup.3 is nitro, amino, C.sub.1 -C.sub.4 -alkanoylamino or benzoylamino, andR.sup.4 is a radical of the formula ##STR2## where X.sup.1, X.sup.2 and X.sup.3 are each hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl or substituted or unsubstituted phenyl, andX.sup.4 is a group which is detachable under alkaline conditions,either in the free form or in the form of their salts, are useful for synthesizing reactive dyes.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: July 6, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Siegel, Claus Marschner, Manfred Patsch
  • Patent number: 5220048
    Abstract: Benzocyclobutene-1,2-dichlorides, -bromides and -iodides which are substituted in the benzene ring are accessible in good yields and short reaction times by reacting substituted 1,2-(dichloromethyl or dibromomethyl)-benzenes with NaI in acetonitrile as the solvent. They can be used together with dienophils, for example 1,4-quinones, in Diels-Alder reactions.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: June 15, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Marcus Baumann, Walter Fischer, Vratislav Kvita, Carl W. Mayer
  • Patent number: 5210257
    Abstract: Novel aryl ethers, containing both a carboxylic acid and a sulfonic acid functionality; and a process for making them are described. These difunctional aryl compounds comprise:i) a carboxylic acid group or its derivative,ii) a first aromatic group bonded to the carboxylic acid or its derivative,iii) a second aromatic group linked to the first aromatic group by a non-electron-withdrawing moiety,iv) a third aromatic group linked to the second aromatic group by a non-electron-withdrawing moiety, andv) a sulfonyl group or its derivative bonded to the third aromatic group.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: May 11, 1993
    Assignee: The Dow Chemical Company
    Inventor: William J. Harris
  • Patent number: 5206428
    Abstract: A tetrahydronaphthalene derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group, naphthyl group, a sulfur- or nitrogen-containing heterocyclic group, a lower alkyl group or cycloalkyl group, and R.sup.2 is hydroxymethyl group, carboxyl group, a lower alkoxycarbonyl group or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or a lower alkyl group, R.sup.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: April 27, 1993
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Hideo Nakai, Toyoharu Yamashita, Harumichi Kohno, Yasuhiko Sasaki, Akio Odawara
  • Patent number: 5196576
    Abstract: A chelating compound of the formula:(R-NHOC-CH.sub.2).sub.n --A--(CH.sub.2 COOH).sub.m (I)wherein R is an aromatic ring-containing organic group, A is a residue of an aminopolyacetic acid excluding acetic acid groups (--CH.sub.2 COOH) therefrom, m is an integer of at least two and n is an integer of 1 or 2, or its salt, which has a specificity to a hepatobiliary system so that a complex formed between said chelating compound and a metallic element through a covalent bond is useful as a diagnostic or therapeutic agent for hepatobiliary organs and tissues.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: March 23, 1993
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Shigemi Seri, Hirohiko Yamauchi, Makoto Azuma, Yoji Arata
  • Patent number: 5189211
    Abstract: A sulfonamide derivative represented by the Formula: ##STR1## wherein A, B, X, Y, R, m and n are as defined in the specification, and a salt thereof have thromboxane A.sub.2 antagonism, therefore they are useful, for example, as blood platelet aggregation inhibiting agents.
    Type: Grant
    Filed: July 26, 1991
    Date of Patent: February 23, 1993
    Assignees: Taisho Pharmaceutical Co., Ltd., Nippon Suisan Kaisha, Ltd.
    Inventors: Masakazu Sato, Yutaka Kawashima, Jun Goto, Yoshiyuki Chiba, Mikio Satake, Chuzo Iwata, Takeshi Imanishi
  • Patent number: 5179125
    Abstract: Novel N-substituted mercaptopropanamide derivatives of the formula: ##STR1## wherein R.sub.1 is mercapto or a group convertible into mercapto when cleaved within the biobody, W is hydrogen atom, an alkyl or an aralkyl, R.sub.2 is an aryl which may optionally have substituent(s), a heterocyclic group which may optionally have substituent(s), or an alkyl which may optionally have substituent(s), X is a cycloalkylene, a cycloalkylidene, or a phenylene which may optionally have substituent(s) or may optionally be fused with other ring, and R.sub.3 is carboxyl or a group convertible into carboxyl when cleaved within the biobody, or a pharmaceutically acceptable salt thereof, and a solid solution of said N-substituted mercaptopropanamide derivative with an amino acid, which have excellent enkephalinase inhibitory activity and are useful for the treatment of mild to moderate pain, and a pharmaceutical composition containing said compounds as an active ingredient, and processes for preparing these compounds.
    Type: Grant
    Filed: April 4, 1990
    Date of Patent: January 12, 1993
    Assignee: Dainippon Pharmaceutical Co., Ltd.
    Inventors: Tetsutaro Mimura, Yasuhisa Nakamura, Junko Nishino, Tadahiro Sawayama, Takashi Sasagawa, Takashi Deguchi, Hideo Nakamura
  • Patent number: 5177069
    Abstract: The present invention provides a novel class of naphthylsulfonylalkanoic acid compounds such as a structure corrresponding to the formula: ##STR1## or a pharmaceutically acceptable salt thereof. A present invention naphthylsulfonylalkanoic acid compound is useful for prevention or treatment of irritable bowel syndrome, biliary dyskinesia and acute pancreatitis.
    Type: Grant
    Filed: December 6, 1990
    Date of Patent: January 5, 1993
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Makio Kitazawa, Masuo Akahane, Yasushi Nakano, Atsushi Tsubaki, Kazuaki Sato, Masaaki Ban, Michihiro Kobayashi
  • Patent number: 5152921
    Abstract: Liquid detergents containing, as the fluorescent whitener, 2,2'-dichloro-5,5'-disulfodistyrylbiphenyl, process for the preparation and use of the liquid detergent for washing and pre-treating textile fabrics; these are liquid detergents which are stable on storage, do not sediment, are stable to bleaching systems and do not form spots in the course of pre-treatment.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: October 6, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Weber, Claude Eckhardt
  • Patent number: 5153352
    Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occuring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein R.sub.24 is the side chain of any of the naturally occuring amino acids, --CH.sub.1 SH, --Ch.sub.2 Cl, --Ch.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: October 6, 1992
    Assignee: Bristol-Myers Squibb Company
    Inventors: Daniel W. Norbeck, Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin
  • Patent number: 5153227
    Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
  • Patent number: 5149859
    Abstract: A naphthalene derivative having the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or a non-toxic salt moiety; R.sup.2 and R.sup.3 independently represent a hydrogen atom or --OR.sup.4 where R.sup.4 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group;A represents a group: ##STR2## [where X.sup.1 and X.sup.2 represents an oxygen atom or N--OR.sup.5 (where R.sup.5 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], a group: ##STR3## [where Y.sup.1 and Y.sup.2 independently an oxygen atom or a group N--OR.sup.6 (where R.sup.6 represents a hydrogen atom or a C.sub.1 -C.sub.3 alkyl group)], or a group: ##STR4## (where n is 0 or 1); and B represents --(CH.sub.2).sub.m --wherein m is an integer of 1, to 8,--(CH.sub.2).sub.m.sbsb.1 --O--(CH.sub.2).sub.m.sbsb.2 --wherein m.sub.1 and m.sub.2 are independently 1 or 2, or ##STR5## wherein m.sub.3 is 0 or 1.
    Type: Grant
    Filed: September 14, 1990
    Date of Patent: September 22, 1992
    Assignee: Teijin Limited
    Inventors: Atsuo Hazato, Takumi Takeyasu, Koji Tomimori, Yoshinori Kato
  • Patent number: 5145867
    Abstract: Naphthylalkylamino-substituted sulfamoylbenzoic acid derivatives, processes for the preparation thereof and the use thereof as medicines.Compounds I ##STR1## R(1) hydrogen, (C.sub.1 -C.sub.4)-alkyl and Na, K, NH.sub.4, Ca, Mg, R(2) and R(3) hydrogen, alkyl groups which can also be linked together in a ring,X oxygen, sulfur, SO, SO.sub.2, NR(6) [with R(6)=hydrogen-alkyl], CH.sub.2, CO, or a bond,R(4) phenyl, thienyl, which are unsubstituted or substitutedR(5) hydrogen, (C.sub.1 -C.sub.4)-alkyl,n 1, 2, 3 or 4,where the naphthyl system is unsubstituted or substituted like the phenyl radical of R(4),and where X and R(4) together can also be Cl are medicaments for treating sickle-cell anemia.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: September 8, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: John C. Ellory, Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Wulf Merkel
  • Patent number: 5136098
    Abstract: Sulfonic acids are reacted with sodium nitrite to form new compositions specifically nitrosyl sulfonates. The nitrosyl sulfonates are useful in reacting with a dye base to form a diazo composition which can in turn react with a coupling agent to form a diazo dye. The nitrosyl sulfonate can also be used to react with an aromatic composition to nitrosoate an aromatic composition. These reactions are particularly useful in the formation of a dispersed dye because the dye can be formed directly in a nonpolar organic solvent and can be used without purification of the dye product. Particularly useful is the nitrosyl dodecyl benzene sulfonate since the formed product is soluble in nonpolar solvents and all reaction products remain in solution and aid with the dyeing of fabrics.
    Type: Grant
    Filed: February 1, 1991
    Date of Patent: August 4, 1992
    Inventor: Rodger L. Gamblin
  • Patent number: 5126462
    Abstract: Aromatic tetracarboxylic acids or derivatives thereof of the general formula I ##STR1## in which R denotes a divalent radical of the formula II ##STR2## Ar denotes tri- or tetravalent aromatic radicals or mixtures thereof, X, if Ar is trivalent, denotes an amide radical, and if Ar is tetravalent denotes an imide radical, and Y and Z either together denote the anhydride radical --CO--O--CO-- or by themselves and independently of one another denote the radicals --COOH, --COCL or --COOR.sub.1, and a process for their preparation.
    Type: Grant
    Filed: June 12, 1990
    Date of Patent: June 30, 1992
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Gerd Greber, Heinrich Gruber, Marcel Sychra
  • Patent number: 5124462
    Abstract: A process for preparing a compound of Formula (I): ##STR1## wherein R' is optionally protected --CH.sub.2 OH or --COOH; R.sup.2 is phenyl or substituted phenyl; and Y is oxygen, methylene, or substituted methylene, which comprises treating a norbornyl acid amide of formula (II): ##STR2## wherein R is optionally protected --CH.sub.2 OH or --COOR.sup.1 ; R.sup.1 is hydrogen or ester-forming group; and Y is oxygen, methylene, or substituted methylene under the reaction conditions for the Hofmann Rearrangement, and then with a substituted sulfonyl halide of formula (III):R.sup.2 SO.sub.2 X (III)wherein R.sup.2 is phenyl or substituted phenyl; and X is halogen atom.
    Type: Grant
    Filed: June 18, 1991
    Date of Patent: June 23, 1992
    Assignee: Shiongi & Co., Ltd.
    Inventors: Mitsuaki Ohtani, Takaharu Matsuura, Yoshinori Hamada, Shoji Shinomoto
  • Patent number: 5118710
    Abstract: Acrylic esters of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or alkyl, X is S, SO or SO.sub.2, R.sup.3 is phenyl, naphthyl or phenanthrenyl, these radicals being unsubstituted or substituted, with the exception of compounds in which R.sup.3 is phenyl, 3-chlorophenyl, 4-chlorophenyl, 2,4-dichlorophenyl or methylphenyl, and fungicides containing these compounds.
    Type: Grant
    Filed: December 31, 1990
    Date of Patent: June 2, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Horst Wingert, Hubert Sauter, Franz Schuetz, Bernd Wenderoth, Siegbert Brand, Bernd Mueller, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5106870
    Abstract: This invention relates to several thromboxane A.sub.2 inhibiting 7-[3-.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-bicyclo[2.2. 1]-heptenoic acids, pharmaceutical compositions employing them and methods of their use.
    Type: Grant
    Filed: September 10, 1990
    Date of Patent: April 21, 1992
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5100917
    Abstract: The present invention relates to novel A-nor-steroid-3-carboxylic acid derivatives and to their use as inhibitors of mammalian 5.alpha.-reductase.
    Type: Grant
    Filed: September 11, 1990
    Date of Patent: March 31, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Philippe Bey, Thomas R. Blohm
  • Patent number: 5098613
    Abstract: This invention provides benzene derivatives, pharmaceutical formulations of those derivatives, and a method of using the derivatives for the treatment of inflammation in mammals.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: March 24, 1992
    Assignee: Eli Lilly and Company
    Inventors: Nancy G. Bollinger, Theodore Goodson, Jr., David K. Herron
  • Patent number: 5091564
    Abstract: Disclosed is a process for preparing a diphenyl sulfonetetracarboxylic acid, the process comprising oxidizing a tetramethyldiphenyl sulfone with oxygen or an oxygen-containing gas in an aliphatic monocarboxylic acid having 2 to 10 carbon atoms in the presence of a catalyst consisting essentially of a cobalt component, a manganese component and a bromine compound wherein the weight ratio of manganese metal to cobalt metal is in the range of approximately 0.01 to 0.5.
    Type: Grant
    Filed: September 20, 1990
    Date of Patent: February 25, 1992
    Assignee: New Japan Chemical Co., Ltd.
    Inventors: Hiroshi Manami, Mikio Nakazawa, Shigeo Miki, Akihiro Nishiuchi
  • Patent number: 5087743
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: February 11, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5081282
    Abstract: Bicyclo prostaglandin analogues have been prepared.
    Type: Grant
    Filed: January 13, 1988
    Date of Patent: January 14, 1992
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5047425
    Abstract: Compounds of the formula ##STR1## wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the meanings mentioned in the description, processes and intermediates for their preparation, pharmaceutical compositions which contain them and their use in therapy in the treatment of cardiovascular diseases.
    Type: Grant
    Filed: November 30, 1988
    Date of Patent: September 10, 1991
    Assignee: Simes Societa Italiana Medicinali & Sintetici SpA
    Inventors: Cesare Casagrande, Francesco Santangelo, Luisa Calabi
  • Patent number: 5041635
    Abstract: There is provided 5(Z)-7-(endo-3-benzenesulfonamidobicyclo[2.2.1]hept-exo-2-yl)-5-heptenoic acid, sodium salt which is useful as an antithrombotic, anti-vasoconstricting and anti-bronchoconstricting agent.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: August 20, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani
  • Patent number: 5030653
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: July 9, 1991
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5023268
    Abstract: Compounds related to 3-phenoxy (or phenylthio) cyclopentanecarbonylamino acid, processes for their preparation, and treating agents for cerebral edema containing the compounds as active ingredients are described. The compounds are represented by the following formula: ##STR1## The compounds of the present invention and their non-toxic salts have a potent inhibitory effect on the development of cerebral edema.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: June 11, 1991
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Katsuhiro Imaki, Tadao Okegawa, Yoshinobu Arai
  • Patent number: 5017583
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: February 23, 1988
    Date of Patent: May 21, 1991
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
  • Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 5013861
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.
    Type: Grant
    Filed: October 6, 1986
    Date of Patent: May 7, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 5010104
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5008430
    Abstract: The invention relates to mercaptopyrenes of the formula ##STR1## in which n denotes a whole number from 3 to 10 andR stands for a substitute or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or aryl radicalto a process for its preparation, its use for the preparation of CT complexes and to the CT complexes obtained.
    Type: Grant
    Filed: April 10, 1989
    Date of Patent: April 16, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Heywang, Friedrich Jonas
  • Patent number: 5006542
    Abstract: Arylthioalkylphenylcarboxylic acids 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 where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## where R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasopastic diseases.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: April 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Patent number: 5004817
    Abstract: Compounds having the formula (I): ##STR1## wherein: M is an alkali or alkaline-earth metal or a C.sub.1 -C.sub.18 alkyl group;X is a group selected from --CH.sub.2 --, --CO--, --CH.sub.2 --CO--, --CH(CH.sub.3)--CO--,p is 0 or 1;Ar is a simple or condensed aromatic ring or Ar represents two or more aromatic nuclei bonded either by a simple bond or by an --O--, --S--, --SO.sub.2 --, --SO--, --CO--, --CS--, or --NH-- group;y is H or CH.sub.3 ;m is 1 when Y=--CH.sub.3, or an integer from 1 to 5 (including both values) when Y=H; n is a number ranging from 1 to 500 (including both values); andZ is H; a C.sub.1 -C.sub.18 alkyl; benzyl; glycidyl; acetyl; allyl; --CO--NH--R or --CO--NH--R.sub.1 --NCO group.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: April 2, 1991
    Assignee: Montefibre, S.p.A.
    Inventors: Catia Bastioli, Salvatore Garlisi, Dario Fornara, Vittorio Bellotti
  • Patent number: 4996352
    Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.- hydroxy-4-methoxybenzenepropanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin- 4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: February 26, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erno Mohacsi
  • Patent number: 4994494
    Abstract: Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.
    Type: Grant
    Filed: December 14, 1989
    Date of Patent: February 19, 1991
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: John R. Regan, Joseph G. Bruno, Kent W. Neuenschwander, Donald E. Kuhla
  • Patent number: 4992581
    Abstract: This invention relates to several novel methods of manufacturing thromboxane A.sub.2 inhibiting 7-[3-.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-bicyclo[2.2. 1]-heptenoic acids.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: February 12, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 4992563
    Abstract: This invention relates to several intermediates useful in preparing thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-1.alpha ., 4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha., 7a.alpha.-4.alpha.,7.alpha.-methano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: February 12, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 4990660
    Abstract: Aromatic hydroxycarboxylic acids of the formula(HO--).sub.n A--COOHwhere n is 1 or 2 and A is a radical from the benzene, naphthalene, biphenyl, diphenyl ether, diphenyl sulfide or diphenyl sulfone series, are prepared by a process in which an acylated aromatic compound of the formula(R.sup.1 --CO--O--).sub.n A--CO--R.sup.2where R.sup.1 and R.sup.2 independently of one another are each unsubstituted or substituted C.sub.1 -C.sub.4 -alkyl and n and A each have the abovementioned meanings, is oxidized with oxygen in the presence of a catalyst and of a solvent at from 20.degree. to 250.degree. C. to give a carboxylic acid of the formula(R.sup.1 --CO--O--).sub.n A--COOHwhere R.sup.1, n and A have the abovementioned meanings, and the acyl group or groups is or are then eliminated.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: February 5, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Neumann, Ulrich Eichenauer
  • Patent number: 4983628
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reaction substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: January 3, 1989
    Date of Patent: January 8, 1991
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
  • Patent number: 4980372
    Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein R.sup.1 represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s),A represents oxygen atom, sulfur atom or sulfinyl (SO) group, two R.sup.1 s represents methyl groups or chlorine atoms at the same time or cyclopentane, cyclohexane or benzene ring together with the carbon atoms of benzene ring each attaching,R.sup.2 represents a group of general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula:NR.sup.11 (wherein R.sup.11 represents hydrogen atom or alkyl group of from 1 to 4 carbon atom(s)),R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s) halogen atom, trifluoromethyl group or cyclobutylmethyl group,m represents 0 or 1,n represents an integer of from 1 to 5, andR.sup.9 and R.sup.
    Type: Grant
    Filed: May 6, 1988
    Date of Patent: December 25, 1990
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
  • Patent number: 4976891
    Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted arly, aralkyl or hetelocycle; R.sub.3 is hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkeneylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Sanji Hagishita, Kaoru Seno, Susumu Kamata
  • Patent number: 4975444
    Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.
    Type: Grant
    Filed: August 25, 1989
    Date of Patent: December 4, 1990
    Assignee: Pfizer Inc.
    Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
  • Patent number: 4973604
    Abstract: This invention relates to several thromboxane A.sub.2 inhibiting 7-[3-.alpha.-[1-[[(phenylamino)-thioxomethyl]hydrazono]ethyl]-bicyclo[2.2. 1]-heptenoic acids, pharmaceutical compositions employing them and methods of their use.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: November 27, 1990
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 4970336
    Abstract: This invention relates to methods of preparing and purifying .alpha.-substituted acetic acids, which comprise treating an .alpha.aromatic-substituted acetic acid represented by a specific general formula with a weak alkali while shielding light, or subjecting an .alpha.-aromatic-substituted acetonitrile represented by a specific general formula to acid hydrolysis, followed by treatment with a weak alkali while shielding light; and treating the alkali salt of .alpha.-substituted acetic acid thus formed with a decolorizing agent.
    Type: Grant
    Filed: May 31, 1989
    Date of Patent: November 13, 1990
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yoshikazu Yoshioka, Isao Hashiba, Suketoshi Tsukamoto