At Least Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/117)
  • Patent number: 5302596
    Abstract: Novel tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting activity and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: April 12, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5290936
    Abstract: A novel chemiluminescent labeling compositions comprising an ester, thiolester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinguished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with --NO.sub.2 meta or para substituents thereon.
    Type: Grant
    Filed: March 30, 1992
    Date of Patent: March 1, 1994
    Assignee: London Diagnostics, Inc.
    Inventors: Iraj Beheshti, Harlen Koelling
  • Patent number: 5256661
    Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.
    Type: Grant
    Filed: September 28, 1992
    Date of Patent: October 26, 1993
    Assignee: Whitby Research, Inc.
    Inventor: Alan S. Horn
  • Patent number: 5248681
    Type: Grant
    Filed: September 19, 1991
    Date of Patent: September 28, 1993
    Assignee: Pfizer Inc.
    Inventor: Kelvin Cooper
  • Patent number: 5244896
    Abstract: This invention relates to novel carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.
    Type: Grant
    Filed: January 23, 1992
    Date of Patent: September 14, 1993
    Assignee: Marion Merrell Dow Inc.
    Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
  • Patent number: 5240937
    Abstract: This invention describes the preparation and use of anticonvulsant agents. In particular, triazolopyridine compounds are described which have utility in the treatment of epilepsy in mammals.
    Type: Grant
    Filed: May 1, 1992
    Date of Patent: August 31, 1993
    Assignee: Burroughs Wellcome Co.
    Inventor: James L. Kelley
  • Patent number: 5232930
    Abstract: The invention concerns a benzodioxole derivative of the formula I ##STR1## wherein Ar.sup.1 is an optionally substituted 9- or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 -- which, together with the carbon atom to which A.sup.1 and A.sup.2 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X is oxy, thio, sulphinyl or sulphonyl, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof;which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: August 3, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: John F. Kingston, David Waterson
  • Patent number: 5214044
    Abstract: The invention provides compounds of the formula: ##STR1## The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic conditions.
    Type: Grant
    Filed: September 18, 1991
    Date of Patent: May 25, 1993
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Michael J. Fray
  • Patent number: 5166209
    Abstract: This invention describes the preparation and use of anticonvulsant agents. In particular, triazolopyridine compounds are described which have utility in the treatment of epilepsy in mammals.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: November 24, 1992
    Assignee: Burroughs Wellcome Co.
    Inventor: James L. Kelley
  • Patent number: 5133798
    Abstract: A compound of formula (I): ##STR1## in which the dotted lines indicate the presence of two double bonds arranged so as to form a fused hetero-aromatic ring system;Ar is an optionally substituted aryl or heterocyclic ring;W is O or NR.sup.1, where R.sup.1 is hydrogen or lower alkyl;X is (CH.sub.2).sub.n, CH.dbd.CH, CH(OR.sup.5)CH.sub.2, COCH.sub.2 ;where n is O, 1 or 2;R.sup.2 and R.sup.3 are independently selected from H, optionally substituted alkyl, alkenyl or alkynyl, halogen, NR.sup.6 R.sup.7 or R.sup.2 and R.sup.3 together with the carbon to which they are attached form an optionally substituted alkenyl or cycloalkyl group;R.sup.4 is CO.sub.2 R.sup.8, CN, COR.sup.8, CH.sub.2 OR.sup.8, CH(OH)R.sup.8, CH(OR.sup.8)R.sup.9, CSNH.sub.2, COSR.sup.8, CSOR.sup.8, CONHSO.sub.2 R.sup.8, CONR.sup.10 R.sup.11, CONHNR.sup.10 R.sup.11, CONHN.sup.+ R.sup.10 R.sup.11 R.sup.12 R.sup.13-, CO.sub.2.sup.- R.sup.14+ or COON.dbd.CR.sup.10 R.sup.11 ;R.sup.14+ is an agriculturally acceptable cation; and R.sup.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: July 28, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: David P. J. Pearson, John E. D. Barton, David Cartwright, Susan P. Barnett
  • Patent number: 5077407
    Abstract: The present invention provides novel substituted 2-[monoannelated(3,4- 4,5-, and 5,6-)pyridylalkylenesulfinyl]-benzimidazoles with gastric acid inhibiting effects.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: December 31, 1991
    Assignee: The Upjohn Company
    Inventor: John C. Sih
  • Patent number: 5039689
    Abstract: The present invention relates to the use of a compound of formula (I) ##STR1## wherein R representsa hydrogen atom; a C.sub.1-4 alkyl group;a group COR.sup.1 wherein R.sup.1 represents amino or C.sub.1-4 alkoxy; ora group --CH.sub.2 R.sup.2 wherein R.sup.2 represents a halogen atom (e.g. chlorine or bromine), C.sub.1-4 alkylthio, or azido,X and Y each independently represent --CH-- or --N; andZ represents --CR.sup.3, wherein R.sup.3 is hydrogen or C.sub.1-4 alkyl, or Z represents --N--;or a physiologically acceptable salt, ester or other physiologically functional derivative thereof,for the manufacture of a medicament for the treatment and/or prophylaxis of a parasitic infection in a mammal, and to certain novel compounds of formula (I), pharmaceutical compositions containing them and processes for their preparation.
    Type: Grant
    Filed: November 8, 1989
    Date of Patent: August 13, 1991
    Assignee: Burroughs Wellcome Co.
    Inventor: Susan M. Daluge
  • Patent number: 5010198
    Abstract: Benzoxazol- and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia. These compounds are produced from certain benzoxazol- and benzothizolamine intermediates.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: April 23, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
  • Patent number: 5001148
    Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: March 19, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Patent number: 4908056
    Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.
    Type: Grant
    Filed: February 17, 1989
    Date of Patent: March 13, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Chi-Ping Tseng
  • Patent number: 4861785
    Abstract: Benzoxazol-and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia.
    Type: Grant
    Filed: October 11, 1985
    Date of Patent: August 29, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
  • Patent number: 4816457
    Abstract: Heterocyclic aminoethanols of the formula:Het--CHOH--CH.sub.2 --NH-aralkylwhere Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: March 28, 1989
    Inventors: John J. Baldwin, Joseph Atkinson, David E. McClure
  • Patent number: 4746676
    Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
    Type: Grant
    Filed: September 12, 1984
    Date of Patent: May 24, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, Paul Menard
  • Patent number: 4720496
    Abstract: Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.
    Type: Grant
    Filed: June 4, 1986
    Date of Patent: January 19, 1988
    Assignee: Boehringer Ingelheim KG
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
  • Patent number: 4698352
    Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: October 6, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
  • Patent number: 4686222
    Abstract: Heterocyclic aminoethanols of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.
    Type: Grant
    Filed: October 3, 1985
    Date of Patent: August 11, 1987
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
  • Patent number: 4568679
    Abstract: Heterocyclic aminoethanols of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals for reducing intraocular pressure, for use as .alpha.- and .beta.-and adrenergic blocking agents, as antihypertensive agents and for effecting bronchodilation.
    Type: Grant
    Filed: March 25, 1982
    Date of Patent: February 4, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
  • Patent number: 4329459
    Abstract: The present invention provides novel 8-heteroaryltetrahydrobenzopyrans and analogs thereof. These novel compounds are useful as inhibitors of endoperoxide cyclooxygenase which prevents the conversion of unsaturated fatty acids to endoperoxides. Because of this pharmacological activity, these compounds represent potent platelet aggregation inhibitors.
    Type: Grant
    Filed: May 5, 1980
    Date of Patent: May 11, 1982
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4266060
    Abstract: The invention relates to compounds of formula: ##STR1## wherein R'.sub.1 =H, OH or an alkyl group, preferably a lower alkyl group, alkylthio or alkoxy, an halogen or an amino group,R'.sub.2 =H or a lower alkyl group.These compounds have antitumoral and antiviral properties useful for the treatment of cancers.
    Type: Grant
    Filed: April 13, 1978
    Date of Patent: May 5, 1981
    Assignee: Agence Nationale de Val orisation de la Recherche (ANVAR)
    Inventors: Emile Bisagni, Claire Ducrocq, Christian Rivalle, Pierre Tambourin, Francoise Wendling, Jean-Claude Chermann, Luc Montagnier
  • Patent number: 4206216
    Abstract: A compound of the formula ##STR1## possesses antihypertensive activity. Also provided are methods for the preparation of the compounds as well as pharmaceutical formulations and methods for their use as antihypertensive agents.
    Type: Grant
    Filed: June 5, 1978
    Date of Patent: June 3, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Joseph G. Atkinson, Clarence S. Rooney, Yves Girard, Edward L. Engelhardt