The Nitrogen Is Part Of A Hetero Ring Patents (Class 514/273)
  • Patent number: 6613773
    Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: September 2, 2003
    Assignee: Syngenta Limited
    Inventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
  • Patent number: 6548512
    Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
  • Patent number: 6512000
    Abstract: A method for treating diseases in which tryptase inhibitors may be of thereapeutic value, which comprises the administration of a thereapeutic amount of a compound of the formula   The invention also comprises novel compounds of the formula (I). Exemplary is 2-[2-(4-amidinophenyl)ethyl]-1-methyl-benzimidazol-5-yl-carboxylic acid-N-(pyridin-3-yl-methyl)-N-methyl-amide-hydrochloride.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: January 28, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Christine Braun, Hans Briem, Bernd Disse, Christoph Hoenke, Hans Michael Jennewein, Georg Speck
  • Patent number: 6500440
    Abstract: The present invention relates to a composition of topical preparation containing alprostadil, which has excellent skin permeation rate with little skin irritation, which is prepared by dissolving alprostadil or a solid dispersion thereof prepared using poloxamer, into a mixture of an oily vehicle, a pyrrolidone and an anti-irritant agent.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: December 31, 2002
    Assignee: Whan In Pharm Co., Ltd.
    Inventors: Sang-Cheol Chi, Dong Soo Lee, Kye Kwan Lee
  • Patent number: 6489347
    Abstract: Compounds of structure (1) are obtained by reduction of compounds of the structures Compounds of structure (1), especially where Z is a hydrogen atom or a 3,4-methylenedioxyphenyl group, are important intermediates for inter alia paroxetine.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: December 3, 2002
    Assignee: SmithKline Beecham plc
    Inventors: Victor Withold Jacewicz, Marvin Sungwhan Yu, Evgeny Shapiro
  • Patent number: 6482829
    Abstract: The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: November 19, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Thierry Godel, Annick Goergler, Torsten Hoffmann, Sabine Kolczewski, Stephan Roever
  • Publication number: 20020143019
    Abstract: A compound of formula (IA) or the pharmaceutically acceptable acid addition salts thereof wherein: R1, R2, R3, R4 and R5 are the same or different and represent hydrogen, halogen, C1-C6alkyl, C1-C4-alkoxy, C1-C4akylthio, hydroxy, 1 amino, mono(C1-C6) alkylamino, di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; R6 is hydrogen or C1-C6alkyl; W is nitrogen, COH, or CH; Y and Z independently represent nitrogen or CH; and A represents an alkylene group of from 2-5 carbon atoms optionally substituted with one or more alkyl groups having from one to four carbon atoms. The compounds of the invention demonstrate high affinity and selectivity in binding to the D4 receptor subtype.
    Type: Application
    Filed: October 23, 2001
    Publication date: October 3, 2002
    Applicant: Neurogen Corporation
    Inventor: Xiao-shu He
  • Patent number: 6432947
    Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: August 26, 1999
    Date of Patent: August 13, 2002
    Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6432963
    Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 13, 2002
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
  • Patent number: 6410726
    Abstract: Salts of pyrimidine derivatives are provided having the formula: wherein R represents hydrogen, methyl or ethyl; Z represents a substituted or unsubstituted 1-piperidinyl, a substituted or unsubstituted 4-morpholinyl, or a substituted or unsubstituted 1-pyrrolidinyl; and Ar represents a substituted or unsubstituted phenyl or a substituted or unsubstituted naphthyl. These salts are particularly useful as antiviral agents (e.g., to treat CMV infections).
    Type: Grant
    Filed: January 8, 2001
    Date of Patent: June 25, 2002
    Assignee: Tularik Inc.
    Inventor: Jay P. Powers
  • Patent number: 6395727
    Abstract: The invention relates to a method of treating non-psychotic disorders by administration of atypical antipsychotic medications, in particular, risperidone. More specifically, the invention relates to a method of treating the eating disorder Bulimia Nervosa and Bulimia-related eating disorders, by administration of antipsychotic medications from the group of compounds designated as atypical antipsychotic mediations. Typical dosage amounts may range from 0.1 milligrams to 4 milligrams per day and may be administered in any dosage forms known in the art, including, but not limited to oral, intramuscular, rectal, transdermal, sustained release forms, controlled release forms, delayed release forms, and response release forms.
    Type: Grant
    Filed: March 17, 2000
    Date of Patent: May 28, 2002
    Assignee: The Cincinnati Children's Hospital Research Foundation
    Inventors: Gina Guadagno, Jodi M. Star
  • Patent number: 6395736
    Abstract: Compositions and methods for the treatment of anorectal disorders are provided in which certain combinations of NO donors, PDE inhibitors, superoxide (O2−) scavengers, &bgr;-adrenergic agonists, cAMP-dependent protein kinase activators, &agr;1-adrenergic antagonists, L-type Ca2+ channel blockers, estrogens, ATP-sensitive K+ channel activators and smooth muscle relaxants are used.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: May 28, 2002
    Assignee: Cellegy Pharmaceuticals, Inc.
    Inventors: Thomas P. Parks, Vivien Mak, Jung-Chung Lee, Charles Lee
  • Patent number: 6391879
    Abstract: A therapeutic solution and application procedure for curing and preventing nail fungus and athlete's foot infections or Onychomycosis comprising a combination of an anti-fungal agent with DMSO in a anhydrous solution of Polyglycol. The DMSO acts as a solvent so that active anti-fungal agents such as Tolnaftate can be delivered directly to fungal infected areas under and around the nail and other areas prone to topical tinea infections. The DMSO, and Tolnaftate dissolved in a viscous solution of polyglycol so that the combined ingredients may be applied directly to the affected areas with superior penetration. The therapeutic solution is formulated by dissolving the Tolnaftate into the DMSO, and then combining the DMSO and polyglycol solutions together to form the therapeutic solution. Repeated applications of the resulting solution on Onychomycosis infected nails over one 4-6 week period yields satisfactory result rates as high as 85-90% without augmenting the therapy with systemic drugs.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: May 21, 2002
    Assignee: Astan, Inc.
    Inventor: Stanley Forrest Reeves
  • Publication number: 20020045635
    Abstract: The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.
    Type: Application
    Filed: July 11, 2001
    Publication date: April 18, 2002
    Inventors: Alfred Binggeli, Hans-Peter Maerki, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
  • Patent number: 6372752
    Abstract: The invention relates to compounds which inhibit the Mycobacterial enoyl-ACP reductase required for cell wall biosynthesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of use of these compounds for treating a bacterial infection in a patient.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: April 16, 2002
    Assignee: Genzyme Corporation
    Inventors: Mark M. Staveski, Scott F. Sneddon, Christopher Yee, Andrew Janjigian
  • Patent number: 6372751
    Abstract: This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: March 30, 2000
    Date of Patent: April 16, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventors: David D. Davey, Gary B. Phillips
  • Patent number: 6358942
    Abstract: A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR1; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are independently H or halo; R5 is H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: March 19, 2002
    Assignee: Pharmacia & Upjohn Company
    Inventors: Richard C. Thomas, Toni-Jo Poel
  • Patent number: 6329379
    Abstract: Racemates, diastereoisomers and optical isomers of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl o
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: December 11, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic
  • Publication number: 20010018436
    Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
    Type: Application
    Filed: December 15, 2000
    Publication date: August 30, 2001
    Applicant: Tularik Inc.
    Inventors: Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
  • Publication number: 20010011094
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: December 27, 2000
    Publication date: August 2, 2001
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Patent number: 6265412
    Abstract: There is provided a composition for external use with a reduced skin irritation comprising minoxidil and 0.01 to 2 parts by weight of at least one antihistaminic agent selected from the group consisting of chlorphenylamine maleate, diphenylimidazole, diphenhydramine and a salt thereof per 1 part by weight of minoxidil.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: July 24, 2001
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Fuminori Kimura, Kenichi Suzuki, Koji Imamura, Takako Okajima
  • Patent number: 6251900
    Abstract: Heterocyclic compounds in which s-triazine or pyrimidine is substituted with benzimidazole and morpholine and which are represented by the Formula I or phermaceutically acceptable acid addition salts thereof: wherein X and Y respectively represent nitrogen atom or one of them represents nitrogen atom and the other represents C—R7 wherein R7 represents hydrogen or halogen atom; R1, R2, R4, R5 and R6 represent hydrogen atom or C1-C6 alkyl; R3 represents morpholino, piperidino, piperazinyl, thiomorpholino, benzimidazolyl, cyano or the like.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Zenyaku Kogyo Kabushiki Kaisha
    Inventors: Seiichiro Kawashima, Toshiyuki Matsuno, Shinichi Yaguchi, Tetsuo Watanabe, Masahiro Inaba
  • Patent number: 6235741
    Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
    Type: Grant
    Filed: May 28, 1998
    Date of Patent: May 22, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Randall W. Hungate, Richard L. Kendall, Ruth Rutledge, Kenneth A. Thomas, Jr., Robert Rubino, Mark E. Fraley
  • Patent number: 6159977
    Abstract: A therapeutic solution and application procedure for curing Nail fungus infections or Onychomycosis comprising a combination of an anti-fungal agent with DMSO in a anhydrous solution of Polyglycol, and including a secondary anti-inflammatory agent. The DMSO acts as a delivery vehicle so that active anti-fungal agents such as Miconazole in combination with an anti-inflammatory compound such as ibuprofen can be delivered directly to fungal infected areas under and around the nail. The DMSO, Miconazole, and ibuprofen are dissolved in a viscous solution of Polyglycol so that the combined ingredients may be applied directly to the affected nails with superior penetration. The therapeutic solution is formulated by dissolving the Miconazole into the Polyglycol over heat and adding the ibuprofen and DMSO over additional heat in a timed process.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: December 12, 2000
    Assignee: Astan, Inc.
    Inventor: Stanley Forrest Reeves
  • Patent number: 6083954
    Abstract: The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl.sup.- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which constitutes a portion of the CFTR protein. The present invention also provides a method of treating CF cells by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound selected by the present inventive identification method. Preferred compounds for such treatment have little or no affinity for adenosine cell receptors. The present invention provides novel compounds useful in practicing the present inventive method, as well as pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 13, 1998
    Date of Patent: July 4, 2000
    Inventors: Harvey B. Pollard, Kenneth A. Jacobson
  • Patent number: 5863924
    Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: January 26, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5852019
    Abstract: The present invention provides a novel compound which is represented by formula (I): ##STR1## wherein preferable examples of R.sup.1 to R.sup.6 are as follows; R.sup.1 and R.sup.2 are each an alkyl group optionally substituted by a halogen atom, an amino group, a hydroxyl group, an alkoxyl group or a thiol group, a hydrogen atom, a halogen atom or an alkoxyl group; R.sup.3 is a hydrogen atom; R.sup.4 is a methyl group; R.sup.5 is a hydrogen atom or an alkyl group; and R.sup.6 is a group of the formula: ##STR2## wherein Z is a phenyl group; and has an antitumor effect.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: December 22, 1998
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Akio Ejima, Masamichi Sugimori, Ikuo Mitsui
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5728706
    Abstract: A benzenesulfonamide derivative of the formula ?I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.
    Type: Grant
    Filed: April 24, 1996
    Date of Patent: March 17, 1998
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, Kosuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5674868
    Abstract: Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH-- (b) or --CH.dbd.CH--C(Cl).dbd.CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.
    Type: Grant
    Filed: June 16, 1995
    Date of Patent: October 7, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges Henri Paul Van Daele, Jean-Paul Rene Marie Andre Bosmans, Willy Joannes Carolus Van Laerhoven
  • Patent number: 5627200
    Abstract: This invention relates to methods for treating intestinal motility disorders, intestinal ulcerations, including inflammatory bowel disease, ulcerative colitis, Crohn's disease and proctitis, and gastrointestinal ulcerations, depression, prostate disease and dyslipidemia by administering a .beta..sub.3 -adrenoceptor antagonist or agonist.
    Type: Grant
    Filed: September 26, 1994
    Date of Patent: May 6, 1997
    Assignee: Pfizer Inc
    Inventors: David K. Kreutter, Robert L. Dow
  • Patent number: 5622954
    Abstract: 5-Substituted-2,4-diaminopyrimidines, and agriculturally acceptable salts thereof, when present in insecticidally or acaricidally effective amounts, and with a suitable agricultural carrier, are useful as active ingredients in novel insecticidal and acaricidal compositions. These pyrimidines may be represented by the following formula: ##STR1## wherein Ar is ##STR2## and wherein U is an alkenylene or alkynylene moiety, and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, V, W, X, Y, Z and n are as defined herein; also disclosed and claimed are novel intermediates thereof.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: April 22, 1997
    Assignee: FMC Corporation
    Inventors: Robert N. Henrie, II, Clinton J. Peake, Thomas G. Cullen, Walter H. Yeager, Mary E. Brown, John W. Buser
  • Patent number: 5602168
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 11, 1997
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 5589478
    Abstract: A benzenesulfonamide derivative of the formula [I]: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH2--, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: December 31, 1996
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Koichiro Yamada, K osuke Yasuda, Kohei Kikkawa, Rikako Kohno
  • Patent number: 5541186
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: July 30, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael L offler, Marcel M uller, Werner Neidhart, Henri Ramuz
  • Patent number: 5525604
    Abstract: A 4-aminopyrimidine of the formula (I): ##STR1## wherein A is a bond, C1-4 alkylene or C1-4 oxyalkylene;Y is a bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenylene or phenyl(C1-4)alkylene;Z is a bond or vinylene;R1 is 4-15 membered heterocyclic ring containing one or two nitrogen atom;R2 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one or two of oxygen or one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) C1-4 alkoxy,(iv) hydroxy(C1-4 alkoxy) or(v) hydroxy;R3 is (i) 4-15 membered heterocyclic ring containing one or two nitrogen, one oxygen, one sulfur, or one nitrogen and one sulfur atom,(ii) C4-15 carbocyclic ring,(iii) formula:CH2.dbd.CH(X)--whereinX is halogen.(iv) hydrogen.l is 1 or 2.and some compounds are excluded.and acid addition salts thereof, salts thereof; have inhibitory effect on cGMP-PDE, or additionally on TXA2 synthetase.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: June 11, 1996
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Sung J. Lee, Yoshitaka Konishi, Orest T. Macina, Kigen Kondo, Dingwei T. Yu, Tamara A. Miskowski
  • Patent number: 5500424
    Abstract: The present invention relates to a compound represented by the general formula (I): ##STR1## [wherein R.sup.1 is a lower alkyl group or the like, R.sup.2 is a lower alkyl group or the like, R.sup.3 and R.sup.4, which may be the same or different, are halogen atoms or the like, R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, are halogen atoms or the like, and X is .dbd.N-- or .dbd.CH--] or a pharmacologically acceptable salt thereof, which has inhibitory effect on acyl-CoA:cholesterol O-acyltransferase (ACAT), a process for producing said compound, and uses of said compound.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: March 19, 1996
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masashi Nagamine, Kenji Yamamoto, Kenji Horiuchi, Yoshimitsu Matsui, Masanori Yoshida
  • Patent number: 5500416
    Abstract: A percutaneous absorption promoting agent comprising (A) at least one anionic surfactant and one or two or more of surfactants having a nitrogen atom in the molecule other than anionic surfactants, (B) one or two or more of anionic surfactants and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, (C) one or two or more of surfactants selected from the group consisting of amphoteric surfactant and semi-polar surfactants and at least one nonionic surfactant having a nitrogen atom in the molecule, (D) one or two or more of surfactants selected from the group consisting of nonionic surfactants, amphoteric surfactants, semi-polar surfactants and cationic surfactants having a nitrogen atom in the molecule, and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, or (E) an amine oxide as the active ingredient, and a dermatological preparation containing these percutaneous absorption promoting agent and drug components.
    Type: Grant
    Filed: September 10, 1993
    Date of Patent: March 19, 1996
    Assignee: Shiseido Company Ltd.
    Inventors: Kiyoshi Miyazawa, Tadahiro Chiba, Yuhei Iwata, Uhei Tamura, Isao Murotani, Shuya Tamaki
  • Patent number: 5439916
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: August 8, 1995
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Edmund J. Sybertz
  • Patent number: 5397781
    Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.
    Type: Grant
    Filed: February 11, 1993
    Date of Patent: March 14, 1995
    Assignee: Mochida Pharmaceutical Company, Limited
    Inventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
  • Patent number: 5314892
    Abstract: Fungicidal compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CH; and X is an optionally substituted 3- to 6-membered heterocyclic ring containing at least one trivalent nitrogen atom by which it is attached to the central pyrimidine ring.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: May 24, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, David P. Bacon
  • Patent number: 5292744
    Abstract: The invention relates to the use of certain 1-[2-pyri(mi)dyl]-5-hydroxy-pyrazoles which are characterized by formula (I) given in the description, as microbicides for the protection of industrial materials, and to certain novel 1-[2-pyri(mi)dyl]-5-hydroxy-pyrazoles which are characterised by formula (II) given in the description.
    Type: Grant
    Filed: August 12, 1992
    Date of Patent: March 8, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Sasse, Michael Schwamborn, Peter Wachtler, Monika Frie, Georg-Wilhelm Ludwig, Wilfried Paulus, Hans-Georg Schmitt
  • Patent number: 5234923
    Abstract: Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: August 10, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Michael A. Poss, Karnail S. Atwal
  • Patent number: 5221316
    Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.
    Type: Grant
    Filed: February 19, 1992
    Date of Patent: June 22, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
  • Patent number: 5179098
    Abstract: Fungicidal compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CH; and X is an optionally substituted 3- to 6-membered heterocyclic ring containing at least one trivalent nitrogen atom by which it is attached to the central pyrimidine ring.
    Type: Grant
    Filed: November 20, 1990
    Date of Patent: January 12, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, David P. Bacon
  • Patent number: 5166206
    Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: November 24, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
  • Patent number: 5126352
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treatment allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: June 30, 1992
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
  • Patent number: 5120716
    Abstract: A percutaneous absorption promoting agent comprising (A) at least one anionic surfactant and one or two or more of surfactants having a nitrogen atom in the molecule other than anionic surfactants, (B) one or two or more of anionic surfactants and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, (C) one or two or more of surfactants selected from the group consisting of amphoteric surfactant and semi-polar surfactants and at least one nonionic surfactant having a nitrogen atom in the molecule, (D) one or two or more of surfactants selected from the group consisting of nonionic surfactants, amphoteric surfactants, semi-polar surfactants and cationic surfactants having a nitrogen atom in the molecule, and one or two or more of nonionic surfactants not having a nitrogen atom in the molecule, or (E) an amine oxide as the active ingredient, and a dermatological preparation containing these percutaneous absorption promoting agent and drug components.
    Type: Grant
    Filed: October 5, 1988
    Date of Patent: June 9, 1992
    Assignee: Shiseido Company Ltd.
    Inventors: Kiyoshi Miyazawa, Tadahiro Chiba, Yuhei Iwata, Uhei Tamura, Isao Murotani, Shuya Tamaki
  • Patent number: 5055471
    Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.
    Type: Grant
    Filed: November 15, 1989
    Date of Patent: October 8, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5037826
    Abstract: 1-Substituted naphthyridines and pyridopyrazines are disclosed which are useful in treating allergic reactions, inflammation, peptic uclers and hyperproliferative skin diseases and in suppressing the immune response in mammals. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.
    Type: Grant
    Filed: December 18, 1986
    Date of Patent: August 6, 1991
    Assignee: Schering Corporation
    Inventors: David J. Blythin, Marvin I. Siegel, Sidney R. Smith
  • Patent number: 4707621
    Abstract: The middle value selection circuit includes three high value selection circuits and one low value selection circuit. Each high value selection circuit consists of a pair of first NPN transistors and a first constant current circuit. The emitter of each first NPN transistor of the high value selection circuit is connected to the first constant current circuit and the base of the second NPN transistor of the low value selection circuit. The base of this second NPN transistor is connected to the second constant current circuit and to an output terminal. The collector of the second NPN transistor is connected to its base. The first constant current circuit produces a current whichis twice the output current of the second constant current circuit. Two analog signals having mutually different combination among three input analog signals are applied to the NPN transistors of one high value selection circuit.
    Type: Grant
    Filed: April 24, 1986
    Date of Patent: November 17, 1987
    Assignee: Hitachi, Ltd.
    Inventors: Setsuo Arita, Takao Sato