The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/180)
  • Patent number: 6177454
    Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.
    Type: Grant
    Filed: February 29, 2000
    Date of Patent: January 23, 2001
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takumi Takahashi, Takayuki Suzuki, Tetsuo Matsui
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6046212
    Abstract: This invention relates to chalcone derivatives represented by the following formula (1): wherein A represents a phenyl group, a quinolyl group or the like, W represents a vinylene group or the like, and R.sup.1 to R.sup.5 each independently represent a carboxyl, cyano, alkyloxycarbonyl or like group, or salts of the chalcone derivatives, and also to drugs containing them as effective ingredients. These compounds have excellent cys-LT receptor antagonism, and are useful as antiallergic agents or the like.
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: April 4, 2000
    Assignee: Kowa Co., Ltd.
    Inventors: Maria Elizabeth Zwaagstra, Mingqiang Zhang, Henk Timmerman, Kazuhiro Onogi, Masahiro Tamura, Tsutomu Toma, Yasushi Wada
  • Patent number: 6034246
    Abstract: There are disclosed herein 2-phenylbenzazole compounds having a 3'-substituent and a 4'-NR.sup.2 R.sup.6 substituent in the phenyl group where R.sup.5 and R.sup.6 are each hydrogen or alkyl, or where the $'-NR.sup.5 R.sup.6 substituent is N-acyl (or N-benzoyl). There are also disclosed 2-phenylbenzazole compounds in the form of 4'-N sulphamate salts. Such compounds exhibit significant selective cytotoxic activity in respect of tumor cells and provide potentially useful chemotherapeutic agents for selective treatment of a range of cancers.
    Type: Grant
    Filed: August 28, 1997
    Date of Patent: March 7, 2000
    Assignee: Cancer Research Campaign Technology Limited
    Inventors: Malcolm Francis Graham Stevens, Dong-Fang Shi, Tracey Dawn Bradshaw, Samantha Wrigley
  • Patent number: 6030619
    Abstract: Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease without the risk of evoking autoantibody responses.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: February 29, 2000
    Assignee: Chiron Corporation
    Inventors: Dan M. Granoff, Gregory R. Moe
  • Patent number: 6011045
    Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: January 4, 2000
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 6007865
    Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: December 28, 1999
    Assignees: Alteon Inc., The Picower Institute for Medical Research
    Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
  • Patent number: 5998424
    Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
    Type: Grant
    Filed: June 18, 1998
    Date of Patent: December 7, 1999
    Assignee: DuPont Pharmaceuticals Company
    Inventors: Robert A. Galemmo, Jr., Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J. P. Pinto, James R. Pruitt, Mimi L. Quan
  • Patent number: 5990145
    Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: December 22, 1997
    Date of Patent: November 23, 1999
    Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.
    Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
  • Patent number: 5980779
    Abstract: A process for producing a liquid crystalline compound represented by the following general formula (A): ##STR1##
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: November 9, 1999
    Assignee: Dai Nippon Printing Co., Ltd.
    Inventors: Junichi Hanna, Masahiro Funahashi, Masanori Akada, Masayuki Ando, Yozo Kosaka
  • Patent number: 5942535
    Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: August 24, 1999
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
  • Patent number: 5939415
    Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: August 17, 1999
    Assignee: Merckle GmbH
    Inventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
  • Patent number: 5900426
    Abstract: Benzothiazole derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component possess a lipid lowering activity and are useful pharmaceuticals for the treatment of hyperlipemia. The lipid lowering agents are of the formula: ##STR1## wherein R.sub.1 is halogen, trifluoromethyl, acetamido or --OX.sub.1 ; X.sub.1 is hydrogen, alkyl or acyl; R.sub.2 is hydrogen, halogen, alkyl, hydroxyalkyl, trifluoromethyl, nitro, amino which may be substituted with alkyl or acyl, carboxy which may be esterified with alkyl, or --OX.sub.2 ; X.sub.2 is hydrogen, alkyl, acyl, carboxyalkyl which may be esterified with alkyl; n is an integer from 1 to 3 denoting the number of substituents R.sub.2 ; and plural R.sub.2 may be the same or different when n is 2 or 3; with the proviso that R.sub.1 is a group other than halogen when R.sub.2 is hydrogen.
    Type: Grant
    Filed: March 27, 1996
    Date of Patent: May 4, 1999
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Hiroki Muramoto, Kiyoshi Fukuda, Taisuke Hasegawa, Kaoru Okamoto, Takayuki Kotani
  • Patent number: 5885983
    Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, and X are as defined herein.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: March 23, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Biller, John K. Dickson, Jr.
  • Patent number: 5853703
    Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
    Type: Grant
    Filed: January 18, 1996
    Date of Patent: December 29, 1998
    Assignees: The Picower Institute for Medical Research, Alteon Inc.
    Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
  • Patent number: 5840917
    Abstract: A phosphorylamide derivative represented by the general formula (I): ##STR1## wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: November 24, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoru Oi, Hideaki Nagaya, Nobuhiro Inatomi, Masafumi Nakao, Hidefumi Yukimasa
  • Patent number: 5789428
    Abstract: The present invention provides an amino-acid amide derivative represented by the formula: ##STR1## (wherein R.sup.1 represents a C1.about.C6 alkyl group, a C3.about.C8 cycloalkyl group, or a phenyl group, R.sup.2 represents a hydrogen atom or a methyl group, X represents a halogen atom, a methyl group, a methoxy group, Y represents a C1.about.C6 alkyl group, A represents an oxygen atom, or a sulfur atom, and n represents 0 or an integer from 1 to 3), an agricultural or horticultural fungicide including an effective amount of the same, and a method for killing agriculturally or horticulturally harmful fungi which comprises a step of using a fungicidally effective amount of the amino-acid amide derivative. The present invention provides the amino-acid amide derivatives, which exhibit superior control of plant diseases such as late blight and downy mildew, and which are not harmful chemicals.
    Type: Grant
    Filed: February 3, 1997
    Date of Patent: August 4, 1998
    Assignees: Kumiai Chemical Industry Co. Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
  • Patent number: 5736487
    Abstract: Compounds of formula (I): ##STR1## (wherein: R.sup.1 is optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, or optionally substituted alkylthio; R.sup.2 is hydrogen, optionally substituted alkyl, cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl or a group of formula --YR.sup.7 ; R.sup.3 is optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy group, optionally substituted alkenyl, optionally substituted alkynyl, halogen, nitro or a group of formula --COR.sup.8, wherein R.sup.8 is hydrogen, alkyl, cycloalkyl or alkoxy; R.sup.4 and R.sup.5 are each hydrogen atom or alkyl; R.sup.6 is optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy group, optionally substituted alkenyl, optionally substituted alkynyl, halogen, nitro, or a group of formula --COR.sup.8, as defined above;A, Q and X are each oxygen or sulfur; Y is a group of formula --CO--, --COO--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 CH.sub.2 O--, --CH.sub.2 CH.sub.
    Type: Grant
    Filed: March 7, 1997
    Date of Patent: April 7, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Soji Sugai, Hiroyuki Komai, Noriaki Kudo, Kazuo Sato, Toyokuni Honma, Junji Kadotani, Kiyoshi Koi, Mitsuru Ito
  • Patent number: 5733648
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5714479
    Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 1996
    Date of Patent: February 3, 1998
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
  • Patent number: 5703071
    Abstract: The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: December 30, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Noriie Itoh, Mineo Kunihara, Hiroshi Kushida, William W. McWhorter, Syunji Nomura, Kazunori Ozawa, Mikio Taniguchi, Kazuo Tsuzuki
  • Patent number: 5703092
    Abstract: The present invention provides novel hydroxamic acids and carbocyclic acids and derivatives thereof and to pharmaceutical compositions and methods of use of these novel compounds for the inhibition of matrixmetalloproteinases, such as stromelysin and other matrix metalloproteinases, and also inhibit the production of tumor necrosis factor (TNF), and are therefore useful for the treatment of arthritis and other related inflammatory diseases.
    Type: Grant
    Filed: April 16, 1996
    Date of Patent: December 30, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Chu-Biao Xue, William F. DeGrado, Carl Peter DeCicco, Irina Cipora Jacobson
  • Patent number: 5700819
    Abstract: Unique benzothiazole derivatives which exert superior aldose redactase inhibiting actions are unexpectedly and advantageously useful in the prophylactic and therapeutic treatment of diabetic complications. A benzothiazole derivative compound of the formula (1): ##STR1## wherein X is halogen, R.sup.1 and R.sup.2, which are the same or different, are each independently hydrogen or halogen, A is a methylene group or a sulfur atom, and --B--COOR.sup.3 is a group as defined in the specification; or a pharmaceutically acceptable salt and a pharmaceutical composition comprising the same which is a useful prophylactic or therapeutic agent for the treatment of diabetic complications.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: December 23, 1997
    Assignee: Grelan Pharmaceutical Co., Ltd.
    Inventors: Tomoji Aotsuka, Naoki Abe, Naoki Ashizawa
  • Patent number: 5698364
    Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I) : ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo) alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: December 16, 1997
    Assignee: Agfa-Gevaert, N.V.
    Inventors: Wilhelmus Janssens, Luc Vanmaele
  • Patent number: 5688818
    Abstract: Provision of a succinamic acid compound of the formula (1) ##STR1## wherein R.sup.1 is an alkyl or a lower alkenyl and R.sup.2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase activity-inhibitory in mammals such as human, and show superior safety.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: November 18, 1997
    Assignees: Senju Pharmaceutical Co., Ltd., The Green Cross Corporation
    Inventors: Hiroshi Hosono, Toshiyuki Nishio, Hiromichi Ishikawa, Yoshiyuki Nakamura, Tetsuo Matsui
  • Patent number: 5668158
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl;R.sub.3 represents hydrogen or acyl;R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;R.sub.5 represents hydrogen or lower alkyl; or R.sub.4 and R.sub.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: September 16, 1997
    Assignee: Novartis Corporation
    Inventor: Cynthia Anne Fink
  • Patent number: 5665887
    Abstract: A novel methine compound is disclosed, which contains a rhodanine ring substituted with a linear or branched alkyl, alkenyl, or alkynyl group containing at least one carboxyl group and at least one ester bond, amide bond, or ether bond. The methine compound has excellent stability and dyeing power.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: September 9, 1997
    Assignee: Fuji Photo Film Co., Ltd.
    Inventor: Toyohisa Oya
  • Patent number: 5656261
    Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: August 12, 1997
    Assignees: The Picower Institute for Medical Research, Alteon Inc.
    Inventors: Anthony Cerami, Peter C. Ulrich, Dilip R. Wagle, San-Bao Hwang, Sara Vasan, John J. Egan
  • Patent number: 5631253
    Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: May 20, 1997
    Assignee: Zeneca Limited
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5594144
    Abstract: The present invention provides novel tropolone derivatives of the formula I ##STR1## wherein R.sub.10 is a substituted or unsubstituted piperazinyl or benzothiazolidinyl group, and pharamaceutical compositions thereof. These compounds are useful for the prevention and treatment of ischemic diseases, including cerebrovascular diseases and cardiovascular diseases.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: January 14, 1997
    Assignee: The Upjohn Company
    Inventors: Noriie Itoh, Mineo Kunihara, Hiroshi Kushida, William W. McWhorter, Syunji Nomura, Kazunori Ozawa, Mikio Taniguchi, Kazuo Tsuzuki
  • Patent number: 5587482
    Abstract: The present invention is directed to a dye suitable for spectral sensitization of a photographic element. Specifically, the dye is a compound having the structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each independently represents H; halogen; alkyl of 1-6 carbons; aryl of 6-24 carbons; alkoxy of 1-6 carbons; carbonyl; or sulfonate; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 taken together represent the atoms necessary to complete a six-membered carbocylic ring;R.sup.5 represents hydrogen, alkyl of 1-6 carbons or aryl of 6-24 carbons;R.sup.6, R.sup.7, and R.sup.8 independently represent alkyl 1-6 carbons; aryl of 6-24 carbons; or any pair of R.sup.6, R.sup.7 and R.sup.8 taken together represent a five- or six-member heterocyclic ring;X represents O, S, CH.dbd.CH, Se, Te or N--R.sup.10 ;Y represents O, S, or N--R.sup.9 ;Z represents O, S or Se;R.sup.9 represents alkyl of 1-6 carbons; or an aryl of 6-24 carbons;R.sup.
    Type: Grant
    Filed: March 7, 1996
    Date of Patent: December 24, 1996
    Assignee: Sterling Diagnostic Imaging, Inc.
    Inventors: Dietrich M. Fabricius, Ralf H. Harms, James J. Welter
  • Patent number: 5576343
    Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 19, 1996
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
  • Patent number: 5563168
    Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.
    Type: Grant
    Filed: June 16, 1995
    Date of Patent: October 8, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5532257
    Abstract: Production of a benzothiazole compound of the formula (I) ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 and R.sup.3 may be the same or different and each is a hydrogen atom or a halogen atom, R.sup.4 is a hydrogen atom, a halogen atom, a lower alkyl, an alkoxy or an alkyl mercapto and R.sup.5 is a hydrogen atom or a lower alkyl, or a pharmaceutically acceptable salt thereof.The compound of the formula (I) and a pharmaceutically acceptable salt thereof of the present invention have an aldose reductase inhibitory activity in mammals inclusive of human and have superior safety. Accordingly, they are useful as pharmaceutical compositions for the treatment of the complications of diabetes, such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, particularly cataract and neurosis.
    Type: Grant
    Filed: November 25, 1994
    Date of Patent: July 2, 1996
    Assignees: Senju Pharmaceutical Co., Ltd, The Green Cross Corporation
    Inventors: Takema Hase, Takahiro Kumonaka, Chikako Shimizu, Hiroshi Hosono, Tomoji Aotsuka, Yoshiyuki Nakamura, Tetsuo Matsui, Hiromichi Ishikawa
  • Patent number: 5510379
    Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: December 19, 1994
    Date of Patent: April 23, 1996
    Assignee: Warner-Lambert Company
    Inventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
  • Patent number: 5482962
    Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: January 9, 1996
    Assignee: Rohm and Haas Company
    Inventor: Robert E. Hormann
  • Patent number: 5466813
    Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: November 14, 1995
    Assignee: Eastman Kodak Company
    Inventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
  • Patent number: 5463045
    Abstract: Dye-donor element for thermal dye transfer comprising at least one magenta dye having extremely low side absorption in the blue and red regions of the spectrum, said dye corresponding to the general formula (I): ##STR1## wherein R.sup.1 is H, (cyclo)alkyl, or aryl; X represents the atoms completing a heterocycle; Z is an electron-withdrawing group; Y is an electron-withdrawing group or --N(R.sup.2)R.sup.3 ; R.sup.2 and R.sup.3 together represent the atoms completing a heterocycle; or R.sup.2 and R.sup.3 together represent .dbd.C(R.sup.4)R.sup.5, or each of R.sup.2 and R.sup.3 represents (same or different) (cyclo)alkyl, aryl, or an electron-withdrawing group; each of R.sup.4 and R.sup.5 (same or different) represents H, (cyclo)alkyl, aryl, a heterocycle, SO.sub.2 R.sup.6, COR.sup.6, CSR.sup.6, POR.sup.6 R.sup.7, OR.sup.8, NR.sup.8 R.sup.9, SR.sup.8, or R.sup.4 and R.sup.5 together represent the atoms completing an aliphatic ring or a heterocycle, each of R.sup.6 and R.sup.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: October 31, 1995
    Assignee: AGFA-Gevaert, N.V.
    Inventors: Wilhelmus Janssens, Luc Vanmaele
  • Patent number: 5436267
    Abstract: A novel N-phenylcarbamate compound or its salt where possible, which is useful as the active ingredient of a biocidal composition for control of harmful organisms, is represented by the following general formula (I): ##STR1## wherein R.sup.1 is unsubstituted or substituted alkyl; R.sup.2 is H, unsubstituted or substituted alkyl, alkenyl, alkynyl or cycloalkyl, or --COX.sup.1 wherein X.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; Z is --CH.sub.2 S--, --SCH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 SCH.sub.2 --, or --CH.sub.2 O--N.dbd.C(R.sup.4)--; R.sup.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: July 25, 1995
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Terumasa Komyoji, Itaru Shigehara, Norifusa Matsuo, Hiroshi Shimoharada, Takeshi Ohshima, Toshio Akagi, Shigeru Mitani
  • Patent number: 5432186
    Abstract: Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl;R.sub.3 represents hydrogen or acyl;R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;R.sub.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: July 11, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Cynthia A. Fink
  • Patent number: 5412099
    Abstract: Intermediate compounds of formula IIR.sup.3 --CHO (II)wherein R.sup.3 is ##STR1## and R.sup.6 and R.sup.7 are as defined in the specification, are useful to make compounds having cardiovascular activity.
    Type: Grant
    Filed: August 6, 1993
    Date of Patent: May 2, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Horst Boshagen, Jurgen Stoltefuss, Alexander Straub, Rainer Gross, Joachim Hutter, Siegbert Hebisch, Martin Bechem
  • Patent number: 5409945
    Abstract: Compounds characterized generally as benzo-fused thiazolidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiazolidinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sub.q --C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, Robert E. Manning
  • Patent number: 5409835
    Abstract: Fluorescent, calcium-binding probe compounds having visible-light excitation and emission wavelengths, and a method of usage for these probe compounds in making wavelength-ratiometric or intensity-ratiometric measurements of calcium ion concentration in samples. The probe compounds generally relate to a heterocyclic part as bonded to a Ca.sup.2+ binding unit, namely, BAPTA, via an ethylenically unsaturated group; preferred examples of the heterocyclic group include benzothiazole, naphthothiazole, thiaflavin, indolenine, chloroindolenine, methoxybenzothiazole, and methoxyindolenine.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: April 25, 1995
    Assignee: The University of Maryland at Baltimore
    Inventors: Joseph R. Lakowicz, Engin U. Akkaya
  • Patent number: 5389620
    Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: February 14, 1995
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
  • Patent number: 5371084
    Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.
    Type: Grant
    Filed: October 28, 1993
    Date of Patent: December 6, 1994
    Assignee: Zeneca Limited
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5364844
    Abstract: Compounds of formula (I): ##STR1## A is a carbon-carbon bond or C.sub.1 -C.sub.3 alkylene; B is imino group or C.sub.1 -C.sub.2 alkylene; R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, heterocyclic or optionally substituted amino; R.sup.2 is optionally substituted phenyl or optionally substituted naphthyl; R.sup.3 is thiazolyl, isoxazolyl or imidazolyl; R.sup.4 is isopropyl or cyclohexyl; R.sup.5 and R.sup.6 are C.sub.1 -C.sub.4 alkyl, or, together with the carbon atom to which they are attached, C.sub.3 -C.sub.7 cycloalkyl; R.sup.7 is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl group; and R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.
    Type: Grant
    Filed: August 27, 1992
    Date of Patent: November 15, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Yasuhiro Morisawa, Mitsuru Kataoka, Yuichiro Yabe, Hiroyuki Koike, Yasuteru Iijima, Hidekuni Takahagi, Tatsuo Kokubu, Kunio Hiwada
  • Patent number: 5302704
    Abstract: Dyes of formula ##STR1## wherein D is the radical of a diazo component of the benzene or naphthalene series or of the heterocyclic series, R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.2 is phenyl or substituted phenyl, give dyeings of good fastness properties on nitrogen-containing or hydroxyl group containing fibre materials.
    Type: Grant
    Filed: August 3, 1992
    Date of Patent: April 12, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean-Marie Adam, Thomas Eichenberger
  • Patent number: 5288744
    Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein Z is O or S, ##STR5## wherein R.sub.5 is lower alkyl or ##STR6## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: February 22, 1994
    Assignee: Centre International De Recherches Dermatologiques (C.I.R.D.)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 5274072
    Abstract: Provided are certain novel substituted 2(5H)furanone compounds which are useful as ultraviolet/visible light absorbing compounds. Also provided are polyester compositions having such compounds copolymerized therein and shaped or formed articles comprised of such polyester compositions.
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: December 28, 1993
    Assignee: Eastman Kodak Company
    Inventors: Max A. Weaver, James J. Krutak, Clarence A. Coates, Jr., William W. Parham, Wayne P. Pruett, Samuel D. Hilbert
  • Patent number: 5266320
    Abstract: The use of an aminovinyl-substituted heterocyclic compound of the general formula I ##STR1## in which R.sup.1 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, or halogen, and, if more than one radical R.sup.1 are present, these may be the same or different,R.sup.2 denotes cyano or C.sub.1 -C.sub.20 -alkoxycarbonyl or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.1 -C.sub.18 -alkoxy, halogen, cyano, C.sub.1 -C.sub.20 -alkoxycarbonyl, or C.sub.3 -C.sub.6 -cycloalkoxycarbonyl, and, if more than one radical R.sup.3 are present, these may be the same or different,X denotes NH, O or S,m is equal to 1 or 2, andn is an integer from 1 to 5,as a stabilizer for organic materials.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: November 30, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Holderbaum, Alexander Aumueller, Hubert Trauth