Patents Examined by Matthew V. Grumbling
  • Patent number: 6706705
    Abstract: The present invention provides a new compound which shows slow and continuous blood pressure reducing action and is useful as an antihypertensive agent. The invention resides in a quinazoline derivative of the following formula (I) and its pharmaceutically acceptable salt: in which, each of R1 and R2 is H or an alkyl group of 1 to 6 carbon atoms, or R1 and R2 are combined to form an ethylene group; each of R3 and R4 is an alkyl group of 1 to 6 carbon atoms; R5 is a hydrogen atom, a hydroxyl group, an alkyl group of 1 to 6 carbon atoms, or an alkoxy group of 1 to 6 carbon atoms; each of R6 and R7 is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms; and n is 2 or 3. The invention further resides in an antihypertensive agent containing the above compound.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: March 16, 2004
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Koichiro Nishioka, Toshihiro Takahashi, Yutaka Nomura
  • Patent number: 6080745
    Abstract: A class of fused tricyclic heteroaromatic compounds of formula (I) as defined in claim 1 or a salt thereof or a prodrug thereof, containing a fused pyrazole, oxazole or pyrimidine ring are ligands for dopamine receptor subtypes within the body and are therefore of use in the treatment and/or prevention of disorders of the dopamine system, such as schizophrenia.
    Type: Grant
    Filed: March 12, 1996
    Date of Patent: June 27, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Barnaby Davey, Paul David Leeson, Michael Rowley
  • Patent number: 6051588
    Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: April 18, 2000
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 5939268
    Abstract: This invention features methods of synthesizing combinatorial libraries of chemical compounds, and combinatorial libraries of chemical compounds formed by the methods of this invention. Specifically, Diels-Alder chemistry is utilized to generate libraries of diverse molecules which are easily differentially functionalized with various chemical moities and in one aspect are configured to act as non-hydrolyzable peptidomimetics.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: August 17, 1999
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • 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: 5932592
    Abstract: A compound represented by the general formula: ##STR1## wherein Y represents a nitrogen atom or C-G (G represents a carboxyl group which may be esterified); ring R is a nitrogen-containing unsaturated heterocyclic group which may be substituted for; each of rings A and B may have a substituent; n represents an integer from 1 to 4; k represents the integer 0 or 1, or a salt thereof, which serves well as an anti-inflammatory agent, particularly a therapeutic agent for arthritis.
    Type: Grant
    Filed: October 21, 1997
    Date of Patent: August 3, 1999
    Assignee: Takeda Chemical Ind., Ltd.
    Inventors: Takashi Sohda, Haruhiko Makino, Atsuo Baba
  • Patent number: 5932521
    Abstract: Novel 1,3-oxazin-4-one derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.5 are hydrocarbyl radicals which are optionally substituted, and herbicidal compositions comprising the same as active ingredients and their use in controlling the growth of weeds. The compounds can be produced by reacting substituted 1,3-dioxin-4-one derivatives and N-methylene-alkylamine.
    Type: Grant
    Filed: July 22, 1997
    Date of Patent: August 3, 1999
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Atsushi Go, Rika Higurashi, Miki Komine, Yoshimi Tsutsumi, Yoshihiro Usui
  • Patent number: 5922706
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: November 13, 1997
    Date of Patent: July 13, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Tamara Ladduwahetty
  • Patent number: 5922711
    Abstract: A compound of the formula: ##STR1## wherein --X.sup.3 .dbd.X.sup.2 --X.sup.1 .dbd.N-- is a group of the formula: ##STR2## R.sup.1 is hydrogen or halogen, R.sup.2 is halogen,R.sup.3 is hydrogen, nitro, amino optionally having at least one substituent or a heterocyclic group optionally having at least one substituent,R.sup.4 and R.sup.5 are each hydrogen, or halogen,R.sup.6 and R.sup.8 are each hydrogen, halogen, lower alkyl, hydroxy, lower alkylthio, amino optionally substituted with lower alkyl, or lower alkoxy optionally substituted with a substituent selected from the group consisting of hydroxy, lower alkoxy, amino, lower alkylamino and aryl optionally substituted with lower alkoxy,R.sup.7 is hydrogen or lower alkyl,A is lower alkylene, andQ is O or N--R.sup.9 is hydrogen or acyl,provided that R.sup.3 is not hydrogen when X.sup.1 is C--R.sup.6, in which R.sup.6 is hydrogen, andpharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: July 13, 1999
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Teruo Oku, Hiroshi Kayakiri, Shigeki Satoh, Yoshito Abe, Yuki Sawada, Takayuki Inoue, Hirokazu Tanaka
  • Patent number: 5919778
    Abstract: The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1-(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z is ##STR1## R2 being an aryl, a substituted aryl, a cycloalkyl or a heterocyclic group, m being an integer of 1 to 6, R3 being hydrogen or a lower alkyl, R4 being an aryl or a substituted aryl, a cycloalkyl or a heterocyclic group, p being an integer of 1 to 6, provided that the cyclic amide compound is quinazoline-on or quinazoline-dion, R2 and R4 are neither aryl nor substituted aryl. The cyclic amide compound is pharmacologically effective to prevent and treat diseases due to insufficiency of the central choline functions.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 6, 1999
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Masahiro Yonaga, Norio Karibe, Youichi Iimura, Satoshi Nagato, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Takashi Kosasa, Kumi Uchikoshi, Kiyomi Yamatsu
  • Patent number: 5902493
    Abstract: A method for forming accurate micro patterns having a micro dimension smaller than the resolution of a stepper used on a semiconductor substrate, thereby achieving an improvement in the integration degree of the semiconductor device which is ultimately produced.
    Type: Grant
    Filed: November 22, 1996
    Date of Patent: May 11, 1999
    Assignee: Hyundai Electronics Industries Co., Ltd.
    Inventor: Sang Man Bae
  • Patent number: 5893983
    Abstract: A technique for polishing an exposed surface of metal on a substrate to remove defects from mechanical working of metals, such as burrs and pigtails resulting from drilling, and defects from plating, such as nodules and depressions, is provided. The substrate has an exposed metal surface such as copper thereon which is to be treated to remove defects. A planarizing or polishing head, preferably a rotating roller, is provided which is continuously rotating with respect to the substrate, with the head in contact with the metal surface on the substrate. A chemical etchant, essentially free of abrasive material, is continuously supplied to the interface between the metal surface and the head. The treating and polishing continues until the defects have been removed or reduced to an acceptable value. In some instances where significant height reduction is required, thus requiring significant metal removal, several passes of the substrate may be required or a device with multiple heads may be used.
    Type: Grant
    Filed: November 19, 1996
    Date of Patent: April 13, 1999
    Assignee: International Business Machines Corporation
    Inventors: John Joseph Konrad, Voya Rista Markovich, George Frederick Reel, Jose Antonio Rios, Timothy Leroy Wells, Michael Wozniak
  • Patent number: 5889018
    Abstract: The invention relates to anxiolytic pharmaceutical compositions comprising as active ingredient 1-sytrylisoquinoline derivatives of general formula (I), whereinn is 1, 2, 3 or 4;R may be the same or different and represent(s) hydrogen, lower alkyl, lower alkoxy or hydroxy, or two substituents R attached to adjacent carbon atoms may form together an alkylenedioxy group;R.sup.1 represents hydrogen or lower alkyl, andAr stands for an optionally substituted aryl or heteroaryl,Some of the compounds of general formula (I) is known, but the majority thereof has not so far described in the literature.The invention also encompasses the preparation of the new compounds of general formula (I), which comprises reacting a compound of general formula (II) with an aldehyde or general formula (III) in the presence of a condensing agent or an acidic catalyst.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: March 30, 1999
    Assignee: Egis Gyogyszergyar RT.
    Inventors: Gyula Balogh, deceased, Imre Doman, Gabor Blasko, Gyula Simig, Erzsebet Kovacs nee Kaszab, Istvan Gyertyan, Andras Egyed, Istvan Gacsalyi, Andras Bilkei-Gorzo, Katalin Pallagi, Katalin Szemeredi, Klara Kazo nee Daroczi
  • Patent number: 5889002
    Abstract: 1,2,4-Thiadiazine and 1,4-thiazine derivatives represented by the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.
    Type: Grant
    Filed: January 17, 1997
    Date of Patent: March 30, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Flemming Elmelund Nielsen, Holger Claus Hansen, John Bondo Hansen, Tina M.o slashed.ller Tagmose
  • Patent number: 5889006
    Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: March 30, 1999
    Assignee: Schering Corporation
    Inventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
  • Patent number: 5885996
    Abstract: Quinazoline compounds which demonstrate antiproliferative activity, such as antitumor activity, processes of preparing these compounds, pharmaceutical compositions containing these compounds, and the use of these compounds. These compounds inhibit the growth and proliferation of the cells of higher organisms and microorganisms, such as bacteria, yeasts and fungi. Preferred quinazoline compounds are capable of inhibiting the enzyme thymidylate synthase. Effects derived from the inhibition of the enzyme thymidylate synthase include those discussed above.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: March 23, 1999
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Ted M. Bleckman, John Attard, Terrence R. Jones, Michael D. Varney
  • Patent number: 5882537
    Abstract: Disclosed is a method of etching which makes the quantitative analysis possible and easier. In the prior art, chemical plasma etching is mainly by ion bombardment, and the tool used to observe the metal bulk is transmission electron microscopy (TEM), so it is very difficult and complicated to execute quantitative analysis. By using chemical plasma etching, the metal precipitate will be left almost all at the end of etching. Scanning electron microscopy (SEM) is used instead of TEM to perform the quantitative analysis.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: March 16, 1999
    Assignee: United Microelectronic Corp.
    Inventors: Yueh-Feng Ho, Chia-Chieh Yu
  • Patent number: 5883094
    Abstract: This invention relates to novel, pharmaceutically active benzimidazolone derivatives of the formula ##STR1## wherein the dashed line, R.sup.0 through R.sup.6 and X.sup.1 through X.sup.3 are defined as in the specification. These compounds exhibit central dopaminergic activity and are u in the treatment of CNS disorders.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 16, 1999
    Assignee: Pfizer Inc.
    Inventors: Anton F-J. Fliri, Brian T. O'Neill, William S. Faraci, Mark A. Sanner, Stevin H. Zorn
  • Patent number: 5874579
    Abstract: An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 2,4-diaminoquinazoline compound of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.6, R.sup.7, W, X, Y, and Z are as defined herein; methods of using the same; novel 2,4-diaminoquinazolines per se; and intermediates in the preparation thereof.
    Type: Grant
    Filed: May 1, 1996
    Date of Patent: February 23, 1999
    Assignee: FMC Corporation
    Inventors: Robert N. Henrie II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager
  • Patent number: 5874397
    Abstract: The invention relates to a granular detergent builder in the form of cogranules of a mixture of sodium bicarbonate and crystalline sheet silicates of the formula NaMSi.sub.x O.sub.2x+1 *yH.sub.2 O, where M is sodium or hydrogen, x is a number from 1.9 to 4, and y is a number from 0 to 20, whereina) the granular detergent builder contains 5 to 50% by weight of crystalline sheet silicate and 50 to 95% by weight of sodium bicarbonate;b) has a pH of .ltoreq.10 in 1% strength solution in distilled water;c) has a calcium-binding capacity of .gtoreq.150 mg Ca/g (30.degree. German hardness) and a magnesium-binding capacity of .gtoreq.4 mg Mg/g (3.degree. German hardness), andd) has an apparent density of .gtoreq.850 g/l.The invention likewise relates to a process for the production of such a granular detergent builder, and to its use in detergents and cleaners.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: February 23, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Schimmel, Alexander Tapper, Volker Thewes