Ring Nitrogen Is Shared By The Cyclos Of The Bicyclo Ring System (e.g., Tetramisole, Etc.) Patents (Class 514/368)
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Patent number: 5468765Type: GrantFiled: December 23, 1994Date of Patent: November 21, 1995Assignee: Pfizer Inc.Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
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Patent number: 5459147Abstract: The invention relates to substituted benzimidazolyl derivatives of the general formula ##STR1## wherein A and R.sub.a to R.sub.c are defined as in claim 1, the mixtures of position isomers thereof and the salts thereof which have valuable properties.These compounds have valuable pharmacological properties, particularly angiotensin-antagonistic effects and preferably angiotensin-II-antagonistic effects.Type: GrantFiled: May 3, 1994Date of Patent: October 17, 1995Assignee: Dr. Karl Thomae GmbHInventors: Norbert Hauel, Uwe Ries, Berthold Narr, Jacques van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5384325Abstract: Compounds based on heterobicyclic derivatives displaying fungicidal activity, having the general formula (I): ##STR1##Type: GrantFiled: April 25, 1994Date of Patent: January 24, 1995Assignee: Isagro S.r.l.Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Ernesto Signorini, Mario Ferri
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Patent number: 5212192Abstract: The present invention relates to novel 6-aryl-5,6-dihydroimidazo[2,1-b]thiazole derivatives having immunostimulating properties, which are useful for treating humans and warm-blooded animals suffering from disorders and/or diseases wherein the immune system is impaired or suppressed. Processes of preparing said novel compounds and compositions containing the same as active ingredient.Type: GrantFiled: December 19, 1991Date of Patent: May 18, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Leopold F. C. Roevens, Willy J. C. Van Laerhoven, Jean P. F. Van Wauwe
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Patent number: 5135847Abstract: A composition contains levamisole and a substrate for alkaline phosphatase in a high pH buffer including 2-amino-2-methyl-1-propanol. The composition may be included in a kit of materials useful in performing an immunoassay in which intestinal alkaline phosphatase is the label. The invention includes a method for detection of a viral antigen by an immunoassay including intestinal alkaline phosphatase as the label and the composition of the invention to provide stabilized levamisole to inhibit nonintestinal alkaline phosphatase.Type: GrantFiled: November 18, 1988Date of Patent: August 4, 1992Assignee: Becton, Dickinson and CompanyInventor: Randal A. Hoke
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Patent number: 5134150Abstract: A method of inhibiting the 5-lipoxygenase pathway in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a diaryl- substituted imidazole fused to a thiazole pyrrolidine, thiazide or piperidine ring to such animal.Type: GrantFiled: December 4, 1989Date of Patent: July 28, 1992Assignee: SmithKline Beecham CorporationInventors: Paul E. Bender, John G. Gleason, Don E. Griswold, Nabil Hanna, Ivan Lantos, Kazys A. Razgaitis, Henry M. Sarau, Susan C. Shilcrat
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Patent number: 5116954Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.Type: GrantFiled: August 2, 1989Date of Patent: May 26, 1992Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 5116836Abstract: Novel 3-aryl-pyrrolidine 2,4-dione derivatives of the formula ##STR1## having pesticidal activity.Type: GrantFiled: August 15, 1990Date of Patent: May 26, 1992Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Hermann Hagemann, Andreas Krebs, Albrecht Marhold, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen, Benedikt Becker, Wilhelm Stendel, Christoph Erdelen
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Patent number: 5098919Abstract: A compound represented by the following formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a cyclic alkyl group;R.sub.2 represents a hydroxyl group, an alkoxy group which may have one to three substituents in the alkyl group moiety, an arylthio group which may have one or more substituents in the aryl group moiety, an aryloxy group which may have one or more substituents in the aryl group moiety, an amino group, an alkylamino group or a cyclic amino group which may contain other hetero atoms as ring atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom;R.sub.Type: GrantFiled: July 13, 1990Date of Patent: March 24, 1992Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Norio Suzuki, Atsushi Nakayama, Toru Hosokami, Masashi Hasegawa, Shuichi Yokohama
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Patent number: 5036082Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: April 18, 1990Date of Patent: July 30, 1991Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 4952594Abstract: The administration internally to humans of certain imidazol derivatives, especially 1-(Beta-hydroxyethyl)-2-methyl-5-nitro-imidazole (metgronidazole); N"-cyano-N-methyl-N'-[2[[(5-methyl-1H-imidazol-4-yl) methyl]thio]ethyl]-guanidine (cimetidine); 6-[1-methyl-4-nitro-imidazol-5-yl)thio] purine (azathioprine); L-(-)-2,3,5,6-Tetrahydro-6-phenyl-imidazo[2,1-b]thiazole (levamisole), or salts of the above compounds, is an effective therapeutic treatment for multiple sclerosis, both acute and chronic. The imidazole moeity is theorized to directly inhibit spread of the virus theorized to cause multiple sclerosis. Treatment of multiple sclerosis with metronidazole with one bolus dose on a frequency of once a day or less and with cimetidine on a frequency of twice per day has been found to be highly efficatious with minimal suppression of the patient's natural immune system and minimal long term peripheral nerve damage.Type: GrantFiled: June 14, 1988Date of Patent: August 28, 1990Inventor: James B. Mercer
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Patent number: 4880824Abstract: Heterocyclic compounds of formulae (I) and (II): ##STR1## where R.sup.1 and R.sup.2 are alkyl, R.sup.3 is H or alkyl, m is 2-5 and Het is a hetercycle such as thiazole, benzothiazole, substituted benzothiazole, pyrazine, triazine, thiadiazole, substituted thiadiazole, pyrimidine or substituted pyrimidine. The compounds are calcium channel blockers useful in the treatment of cardiovascular conditions such as hypertension or angina.Type: GrantFiled: September 21, 1987Date of Patent: November 14, 1989Assignee: Ortho Pharmaceutical CorporationInventors: Jeffery B. Press, Maud Urbanski
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Patent number: 4879293Abstract: The compound of the formula ##STR1## wherein X is a cyclic group which may optionally be substituted; Y is a carboxyl group which may optionally be esterified or amidated; Z is --CH.dbd.CH--CH.dbd.CH--, --S--(CH.sub.2).sub.l --S-- is an integer of 1 to 3), --N.dbd.CH--CH.dbd.N-- or --(CH.sub.2).sub.m --(m is an integer of 3 to 5); ring A may optionally be substituted with halogen, nitro, amino, alkanoylamino, alkoxycarbonyl, carboxyl or carbamoyl; and n is an integer of 1 to 3, and salts thereof. The compounds display a strong antianxiety effect to mammalian animals and are useful for the prevention or treatment of a disease such as psychoromatic disease and anxiety neurosis.Type: GrantFiled: September 8, 1988Date of Patent: November 7, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Kentaro Hiraga, Yoshiaki Saji
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Patent number: 4857539Abstract: Compounds of the formula ##STR1## wherein: Y is an alkylene bridge of 3-9 carbon atoms;Z is N or HC;R is hydrogen or lower-alkyl of 1-5 carbon atoms, with the proviso that when Z is N, R is lower-alkyl;R.sub.1 and R.sub.2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; andHet is selected from specified heterocyclic groups,are useful and antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.Type: GrantFiled: June 16, 1987Date of Patent: August 15, 1989Assignee: Sterling Drug Inc.Inventors: Guy D. Diana, Philip M. Carabateas
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Patent number: 4853402Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.Type: GrantFiled: February 26, 1987Date of Patent: August 1, 1989Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4794120Abstract: Nitrofuran derivatives of formula (I) ##STR1## in which n is 0 or 1 and R is a selected heterocyclic radical have useful antibacterial, antiparasitic and antifungal activity.Type: GrantFiled: July 7, 1987Date of Patent: December 27, 1988Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Michel Aletru
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Patent number: 4735957Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.Type: GrantFiled: November 18, 1986Date of Patent: April 5, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Hisashi Takasugi
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Patent number: 4684658Abstract: The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.Type: GrantFiled: December 20, 1984Date of Patent: August 4, 1987Assignee: Rhone-Poulenc SanteInventors: Jean-Louis Fabre, Daniel Farge, Claude James, Daniel Lave
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Patent number: 4672072Abstract: A pour-on formulation which allows the simultaneous control of internal and external parasites in mammals by a single localized superficial application comprises a pyrethroid in admixture with a thiazole or salt or ester thereof.Type: GrantFiled: March 13, 1985Date of Patent: June 9, 1987Assignee: Wellcome Australia LimitedInventors: Ronald J. Hackney, James J. Guinan
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Patent number: 4657920Abstract: 1,2,4-Triazol-1-yl-methyl-carbinols of the formula ##STR1## in which Ar is optionally substituted aryl, andHet is optionally substituted heteroaryl with at least 2 different hetero-atoms,or addition products thereof with plant-tolerated acids or metal salts, which possess fungicidal activity.Type: GrantFiled: March 22, 1985Date of Patent: April 14, 1987Assignee: Bayer AktiengesellschaftInventors: Jan Gajowski, Erik Regel, Karl H. Buchel, Wilhelm Brandes, Paul Reinecke
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Patent number: 4618618Abstract: The invention concerns novel compounds selected from D,L-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]-thiazolium 4-cyano-2-iodo-6-nitrophenoxide and L-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazolium 4-cyano-2-iodo-6-nitrophenoxide. The compounds are anthelmintics effective against both nematodes and trematodes and in further embodiments the invention provides processes for the preparation of the compounds of the invention, compositions comprising as active ingredient the compounds of the invention and processes for killing helminths using the compounds of the invention.Type: GrantFiled: December 28, 1984Date of Patent: October 21, 1986Inventor: Errol J. McGarry
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Patent number: 4600583Abstract: The method of improving the storage stability of parenterally administerable physiologically active compositions which comprises, incorporating in said compositions a small but effective amount of a compound of the formulae, ##STR1## wherein R is H, lower alkyl or acyl; each R.sup.1 is H or lower alkyl; and n is an integer of from 1 to 6; x is 0 or 1; each Y is H; and the non-toxic pharmaceutically acceptable salts thereof.Type: GrantFiled: September 7, 1982Date of Patent: July 15, 1986Assignee: Tetra Consultants Inc.Inventors: Erik Stevens, Ernestina M. Van Hoeyveld
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Patent number: 4600582Abstract: A method of reducing local adverse reactions which occur at the site of administration of parenterally administrable physiologically active compositions, to patients which comprises, prior to administration thereof, incorporating in said physiologically active compositions, a small but effective amount of a compound of the formulae, ##STR1## wherein n is an integer of from 1 to 6; R.sup.1 is H or lower alkyl; x is 0 or 1; each Y is H; and R is H, lower alkyl or acyl; and the non-toxic pharmaceutically acceptable salts thereof.Type: GrantFiled: September 7, 1982Date of Patent: July 15, 1986Assignee: Tetra Consultants, Inc.Inventors: Erik Stevens, Ernestina M. Van Hoeyveld
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Patent number: 4584305Abstract: Process of aiding regression and palliation of neoplastic disease in animal and human hosts comprising systemic administration to phenylimidazo[2,1-b]thiazole or a nontoxic acid addition salt thereof. Preferably the active ingredient is administered in a sufficient amount to provide dosages over the range from about 1 mg to about 5 mg/kg of body weight of the host.Type: GrantFiled: February 2, 1981Date of Patent: April 22, 1986Assignee: Janssen Pharmaceutica N.V.Inventors: Josephus Brugmans, William Pollack, Paul A. J. Janssen, Daniel Tripodi
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Patent number: 4557932Abstract: The present invention relates to a new compounded composition with synergistic properties, to dosage units thereof, and to the use of the said compounded composition and dosage units.The composition contains as active ingredients the amidinopenicillanic acid mecillinam or a pharmaceutically acceptable, non-toxic salt or pro-drug thereof in combination with another antibiotic compound of the formula ##STR1## or a pharmaceutically acceptable, non-toxic salt or pro-drug thereof, optionally together with pharmaceutically acceptable, non-toxic carriers and/or auxiliary agents.The new composition is valuable in the human and veterinary practice for the treatment of patients suffering from infectious diseases.Type: GrantFiled: December 29, 1982Date of Patent: December 10, 1985Assignee: Leo Pharmaceutical Products Ltd.Inventor: Leif Tybring
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Patent number: 4556669Abstract: Compounds of the formula ##STR1## wherein R is ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are the same or different and are selected from the group consisting of hydrogen, chlorine, bromine, lower alkyl, lower alkoxy and naphthyl, provided that when R.sub.1 is lower alkyl, R.sub.2 and R.sub.3 are hydrogen, chlorine, bromine or lower alkoxy, or a pharmaceutically acceptable salt thereof, have anti-carrageenin edema activity, and are useful as anti-inflammatory agents and immuno modulators. They are produced by reacting an amide of the formula ##STR3## wherein R has the same meanings hereinabove, with N,N'-ethylene thiourea.Type: GrantFiled: April 13, 1984Date of Patent: December 3, 1985Assignees: Kumiai Kagaku Kogyo Kabushiki Kaisha, Toyo Jozo Kabushiki KaishaInventors: Kazuo Nishio, Isao Chiyomaru, Katsuo Anma, Kazuko Yamamoto, Hiroshi Ohno, Noriyasu Takayanagi
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Patent number: 4543358Abstract: This invention relates to aqueous gels, which remain gelatinous in a temperature range as low as -27.degree. C. containing dl- or 1-6-phenyl-2,3,5,6-tetrahydro(-)imidazo[2,1-b]thiazole, acylamino derivatives, thereof and pharmaceutically acceptable salts thereof, characterized by gelation and preparation at ambient temperatures (20.degree.-60.degree. C.), under vacuum, without additional heating or cooling in their preparation.Type: GrantFiled: August 26, 1983Date of Patent: September 24, 1985Assignee: American Cyanamid CompanyInventor: James M. Quinlan
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Patent number: 4536393Abstract: 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.Type: GrantFiled: February 6, 1984Date of Patent: August 20, 1985Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4525357Abstract: Novel derivatives of bicyclic 2-iminothiazolidine oximes and methods of preparing same. This invention is also directed to an insecticidal composition comprising an acceptable carrier and an insecticidally effective amount of a compound of this invention, as well as to a method of controlling insects which comprises subjecting the insects to an insecticidally effective amount of a compound of this invention.Type: GrantFiled: June 24, 1983Date of Patent: June 25, 1985Assignee: Union Carbide CorporationInventors: Dean F. Bushey, Themistocles D. J. D'Silva
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Patent number: 4512998Abstract: Compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms, one of Y and Z is a heterocyclic moiety, and the other of Y and Z is hydrogen, alkyl having 1 to 4 carbon atoms or alkoxy having 1 to 4 carbon atoms are useful as anthelmintics.Type: GrantFiled: October 20, 1980Date of Patent: April 23, 1985Assignee: Schering CorporationInventor: M.Mehdi Nafissi-Varchei