At Least Four Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/117)
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Patent number: 5302596Abstract: 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: GrantFiled: November 23, 1992Date of Patent: April 12, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5290936Abstract: 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: GrantFiled: March 30, 1992Date of Patent: March 1, 1994Assignee: London Diagnostics, Inc.Inventors: Iraj Beheshti, Harlen Koelling
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Patent number: 5256661Abstract: 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: GrantFiled: September 28, 1992Date of Patent: October 26, 1993Assignee: Whitby Research, Inc.Inventor: Alan S. Horn
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Patent number: 5248681Type: GrantFiled: September 19, 1991Date of Patent: September 28, 1993Assignee: Pfizer Inc.Inventor: Kelvin Cooper
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Patent number: 5244896Abstract: 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: GrantFiled: January 23, 1992Date of Patent: September 14, 1993Assignee: Marion Merrell Dow Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
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Patent number: 5240937Abstract: 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: GrantFiled: May 1, 1992Date of Patent: August 31, 1993Assignee: Burroughs Wellcome Co.Inventor: James L. Kelley
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Patent number: 5232930Abstract: 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: GrantFiled: January 9, 1992Date of Patent: August 3, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: John F. Kingston, David Waterson
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Patent number: 5214044Abstract: 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: GrantFiled: September 18, 1991Date of Patent: May 25, 1993Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Michael J. Fray
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Patent number: 5166209Abstract: 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: GrantFiled: October 16, 1990Date of Patent: November 24, 1992Assignee: Burroughs Wellcome Co.Inventor: James L. Kelley
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Patent number: 5133798Abstract: 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: GrantFiled: February 7, 1991Date of Patent: July 28, 1992Assignee: Imperial Chemical Industries PLCInventors: David P. J. Pearson, John E. D. Barton, David Cartwright, Susan P. Barnett
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Patent number: 5077407Abstract: The present invention provides novel substituted 2-[monoannelated(3,4- 4,5-, and 5,6-)pyridylalkylenesulfinyl]-benzimidazoles with gastric acid inhibiting effects.Type: GrantFiled: October 31, 1988Date of Patent: December 31, 1991Assignee: The Upjohn CompanyInventor: John C. Sih
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Patent number: 5039689Abstract: 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: GrantFiled: November 8, 1989Date of Patent: August 13, 1991Assignee: Burroughs Wellcome Co.Inventor: Susan M. Daluge
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Patent number: 5010198Abstract: 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: GrantFiled: August 24, 1989Date of Patent: April 23, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
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Patent number: 5001148Abstract: 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: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4908056Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: February 17, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4861785Abstract: Benzoxazol-and benzothiazolamine derivatives having anti-anoxic properties which compounds are useful in the treatment of anoxia.Type: GrantFiled: October 11, 1985Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel G. M. Luyckx, Frans E. Janssens
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Patent number: 4816457Abstract: 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: GrantFiled: June 30, 1987Date of Patent: March 28, 1989Inventors: John J. Baldwin, Joseph Atkinson, David E. McClure
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Patent number: 4746676Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.Type: GrantFiled: September 12, 1984Date of Patent: May 24, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, Paul Menard
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Patent number: 4720496Abstract: 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: GrantFiled: June 4, 1986Date of Patent: January 19, 1988Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
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Patent number: 4698352Abstract: 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: GrantFiled: October 27, 1983Date of Patent: October 6, 1987Assignee: 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
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Patent number: 4686222Abstract: 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: GrantFiled: October 3, 1985Date of Patent: August 11, 1987Assignees: Merck & Co., Inc., Merck Sharp & Dohme (I.A.) Corp.Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
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Patent number: 4568679Abstract: 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: GrantFiled: March 25, 1982Date of Patent: February 4, 1986Assignee: Merck & Co., Inc.Inventors: Joseph G. Atkinson, John J. Baldwin, David E. McClure
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Patent number: 4329459Abstract: 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: GrantFiled: May 5, 1980Date of Patent: May 11, 1982Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4266060Abstract: 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: GrantFiled: April 13, 1978Date of Patent: May 5, 1981Assignee: 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
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Patent number: 4206216Abstract: 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: GrantFiled: June 5, 1978Date of Patent: June 3, 1980Assignee: Merck & Co., Inc.Inventors: Joseph G. Atkinson, Clarence S. Rooney, Yves Girard, Edward L. Engelhardt