Four Or More Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/251)
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Patent number: 5216159Abstract: The invention encompasses a compound of the formula ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein X, W, Y, R, and R2 are variables.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: November 27, 1991Date of Patent: June 1, 1993Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan J. Hutchison, Vinod Singh
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Patent number: 5212310Abstract: The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## and W, X, A, B, C, D, E, R.sub.3, R.sub.4 are variables. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.Type: GrantFiled: December 19, 1991Date of Patent: May 18, 1993Assignee: Neurogen CorporationInventors: Andrew Thurkauf, Alan Hutchison, Pamela Albaugh
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Patent number: 5210023Abstract: A method of purifying ferment-produced riboflavin, wherein the impure riboflavin is suspended in water or dilute aqueous acid, and the suspension is heated at a temperature of from 75.degree. to 130.degree. C. for from 0.3 to 3 hours with stirring, during which time crystal transformation takes place, after which the mixture is cooled and the purified product is isolated in known manner.Type: GrantFiled: July 1, 1991Date of Patent: May 11, 1993Assignee: BASF AktiengesellschaftInventors: Johannes Grimmer, Hans Kiefer, Christoph Martin
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Patent number: 5196533Abstract: 6,6-Disubstituted pteridines which are useful for the regulation of enzymes are disclosed, along with a general method of synthesizing these compounds.Type: GrantFiled: March 14, 1991Date of Patent: March 23, 1993Assignee: South Alabama Medical Science Foundation, USAInventors: June E. Ayling, Steven W. Bailey
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Patent number: 5180824Abstract: This invention pertains to novel methods of synthesizing fludarabine, fludarabine phosphate and related nucleoside pharmacologic agents utilizing 6-azido-2-fluoropurine as a novel intermediate.In particular this invention pertains to a synthesis of fludarabine where the relatively low yield fluorination step is done before the costly coupling step.Type: GrantFiled: November 29, 1990Date of Patent: January 19, 1993Assignee: Berlex Biosciences Inc.Inventors: John G. Bauman, Randolph C. Wirsching
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Patent number: 5173492Abstract: There are disclosed s-triazolo[3,4-i]purine derivatives represented by formula: ##STR1## wherein Y-Z represents ##STR2## R.sub.4 represents hydrogen, alkyl, substituted or unsubstituted aromatic heterocyclic group or substituted or unsubstituted aryl; and X.sup.2 represents oxygen, sulfur or NH; each of R.sup.1 and R.sup.2 independently represents hydrogen, alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; R.sup.3 represents alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; X.sup.1 represents oxygen or sulfur; and represents a single bond or a double bond or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 23, 1991Date of Patent: December 22, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Fumio Suzuki, Junichi Shimada, Kenji Ohmori, Haruhiko Manabe, Kazuihiro Kubo, Akira Karasawa, Tetsuji Ohno, Shizuo Shiozaki, Akio Ishii, Katsuichi Shuto
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Patent number: 5155112Abstract: The present invention provides the compounds of formula (I) ##STR1## and salts and solvates thereof wherein R.sup.1 represents a hydrogen or fluorine atom or a hydroxy group, R.sup.2 represents a fluorine atom or a hydroxyl or C.sub.1-6 alkoxy group and B represents a purine base, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral infections, particularly those caused by the Herpetoviridae.Type: GrantFiled: November 23, 1990Date of Patent: October 13, 1992Assignee: Glaxo Group LimitedInventors: Richard Storer, Ian L. Paternoster, Alan D. Borthwick, Keith Biggadike
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Patent number: 5132424Abstract: New pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of formula (I), ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and m are as defined in the specification, e.g., 4-(benzoylmethyl)-6-cyclohexyl-6,7-dihydro-2-phenyl-4H-pyrazolo[1,5-a]pyrr olo[3,4-d]pyrimidine-5,8-dione, have been found to be potentially useful to treat warm-blooded animal patients suffering from the symptoms of atherosclerosis and cholesterol buildup to relieve the same and for favorably altering the high density lipoprotein (HDL) to low density lipoprotein (LDL) ratio in blood samples of such patients.Type: GrantFiled: January 21, 1991Date of Patent: July 21, 1992Assignee: The Upjohn CompanyInventors: Scott D. Larsen, Frank P. Bell
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Patent number: 5116843Abstract: The present invention provides tricyclic benzimidazoles of the formula ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or different as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.Type: GrantFiled: June 25, 1990Date of Patent: May 26, 1992Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Erwin Boehm, Klaus Strein
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Patent number: 5110926Abstract: A process is described for the preparation of carbocyclic guanosine from aristeromycin in a multi-step procedure, the final step of which is the hydrolysis of a compound of the formula ##STR1## wherein R.sup.1 represents a C.sub.1-6 alkyl group or an arylC.sub.1-4 alkyl group and R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom or a hydroxyl protecting group.Carbocyclic guanosine is an intermediate in the synthesis of carbocyclic analogues of nucleosides having use in therapy, particularly as antiviral agents.Type: GrantFiled: July 18, 1990Date of Patent: May 5, 1992Assignee: Glaxo Group LimitedInventors: Richard Storer, Chi L. Mo, John P. Turnbull
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Patent number: 5103005Abstract: A method for the recovery of riboflavin from a fermentation broth or other feed stock is disclosed. The method comprises a process for the production of large, pure riboflavin crystals from an alkaline, aqueous solution containing solubilized riboflavin. The method can further comprise the process for production of large, pure riboflavin crystals in combination with two solids/liquid separation steps, the latter of which can result in a final riboflavin product purity of at least about 96% by weight.Type: GrantFiled: July 21, 1989Date of Patent: April 7, 1992Assignee: Coors Biotech, Inc.Inventors: Dale C. Gyure, George W. Lauderdale
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Patent number: 5101032Abstract: Cycloalkylidene dyes have the formula ##STR1## where m is 0 or 1,L is a chemical bond or C.sub.1 -C.sub.2 -alkylene, which may be substituted,R.sup.1 is hydrogen, C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl,Y is oxygen or two hydrogens,X.sup.1 is oxygen andX.sup.2 is C.sub.1 -C.sub.8 -alkanoyloxy, substituted or unsubstituted benzoyloxy, C.sub.1 -C.sub.6 -trialkylsilyloxy or a radical of the formula OR.sup.1 or NR.sup.2 R.sup.3, where R.sup.1 is as defined above and R.sup.2 and R.sup.3 are identical or different and each is independently of the other C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl, or C.sub.3 -C.sub.7 -cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom joining them are saturated heterocyclyl, or else one of R.sup.2 and R.sup.3 is hydrogen, or X.sup.1 and X.sup.Type: GrantFiled: October 22, 1990Date of Patent: March 31, 1992Assignee: BASF AktiengesellschaftInventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel
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Patent number: 5095015Abstract: The invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof where n is 0, 1, or 2 and x is ##STR2## and R.sub.1, R.sub.2, R.sub.3, Y, Z, W, T are defined variables. These compounds are highly selective agonists or inverse agonists for the GABAa brain receptors and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.Type: GrantFiled: July 24, 1990Date of Patent: March 10, 1992Assignee: Neurogen CorporationInventor: Pamela Albaugh
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Patent number: 5095115Abstract: An improved process for preparing riboflavin 5'-phosphate (FMN) or its monosodium salt by reacting riboflavin with excess phosphorus oxychloride in a solvent, hydrolyzing of the resulting reaction mixture and, if desired, partially neutralizing with aqueous sodium hydroxide solution, comprises reacting the riboflavin with from 1.2 to 3 moles of phosphorus oxychloride per mole of riboflavin in a suitable lactone, especially .gamma.-butyrolactone, as solvent. The process is particularly advantageous when the reaction mixture is hydrolyzed at from 80.degree. to 90.degree. C. continuously or batchwise.Type: GrantFiled: August 23, 1990Date of Patent: March 10, 1992Assignee: BASF AktiengesellschaftInventors: Johannes Grimmer, Hans Kiefer
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Patent number: 5086176Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.Type: GrantFiled: June 4, 1991Date of Patent: February 4, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Nelsen L. Lentz
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Patent number: 5079249Abstract: The invention relates to compounds of formula I: ##STR1## in which m=2-4,n and p, which may be identical or different, are an integer equal to 1, 2 or 3, with the proviso that the sum of n and pq=0 or 1,R is a 1,2,3,4-tetrahydro-2,4-dioxo-3-quinazolinyl radical, optionally substituted, a 1,3,4,6,11,11a-hexahydro-1,3-dioxo-2H-pyrazino[1,2-b]isoquinol-2-yl radical, a 1,2-dihydro-1-oxo-2-phthalazinyl radical, optionally substituted, a 2,6-dioxo-1-piperazinyl radical of formula W: ##STR2## (R.sub.3 is a 2-pyridyl radical or an optionally substituted phenyl radical),a radical of formula Z: ##STR3## (R.sub.4 is a carbamoyl radical, a cyano radical, a hydroxycarbonyl radical or an alkoxycarbonyl radical having 1 to 6 carbon atoms),or a radical of formula Y: ##STR4## (R.sub.5 is a 2-pyrimidinyl radical, a 1-isoquinolyl radical, a 2-quinolyl radical, a 2-pyridyl radical, a benzyl radical, optionally substituted, a 2-thiazolyl radical, optionally substituted, or a 2-benzothiazolyl radical) andeither R.sub.1 and R.sub.Type: GrantFiled: August 24, 1990Date of Patent: January 7, 1992Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Francis Colpaert, Michel Laubie
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Patent number: 5070086Abstract: Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of hyperproliferative skin disease are disclosed.Type: GrantFiled: June 15, 1990Date of Patent: December 3, 1991Assignee: Schering CorporationInventor: Richard Friary
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Patent number: 5064826Abstract: This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.Type: GrantFiled: March 2, 1990Date of Patent: November 12, 1991Inventors: Klara Reiter nee Esses, Jozsef Reiter, Zoltan Budai, Endre Rivo, Peter Trinka, Lujza Petocz, Gabor Gigler, Istvan Gyertyan, Istvan Gacsalyi
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Patent number: 5064947Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which can be expected to enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.Type: GrantFiled: June 27, 1990Date of Patent: November 12, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Nelsen L. Lentz
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Patent number: 5032594Abstract: Novel tricyclic fused pyrimidine derivatives of the formula (I): ##STR1## wherein either one of R.sup.1 and R.sup.2 is hydrogen or an optionally substituted aralkyl group and the other is hydrogen, an optionally substituted aralkyl group or an aliphatic hydrocarbon group; R.sup.3 is hydrogen, an aliphatic hydrocarbon group or acyl group; and A is an optionally substituted divalent hydrocarbon chain having 2 to 4 carbon atoms and salts thereof are strong adenosine antagonists and activate cerebral functions and metabolisms, thus being useful as therapeutic or prophylactic agents for neurological or psychic changes caused by cerebral apoplexy, brain injury or cerebral atrophy.Type: GrantFiled: February 15, 1990Date of Patent: July 16, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Naka Takehiko, Nagaoka Akinobu
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Patent number: 5017700Abstract: Riboflavin-4',5'-cyclophosphoric acid chloride of the formula I ##STR1## its preparation by reacting an alkali metal salt of riboflavin, in an aprotic solvent, with phosphorus oxychloride, its use for the preparation of riboflavin-5'-phosphate and of the sodium salt of riboflavin-5'-phosphate, and a process for the preparation of riboflavin-5'-phosphate or its sodium salt via the novel phosphoric acid ester chloride.Type: GrantFiled: September 28, 1989Date of Patent: May 21, 1991Assignee: BASF AktiengesellschaftInventors: Johannes Grimmer, Hans Kiefer
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Patent number: 5013737Abstract: Novel 2,4,8-trisubstituted-3H,6H-1,4,5a,8a-tetraazaacenaphthylene-3,5 (4H)-diones and 2,4,8-trisubstituted-4,5-dihydro-5-thioxo-3H, 6H-1,4,5a,8a-tetra-azaacenaphthylen-3-ones are disclosed which are useful antihypertensive and anxiolytic agents.Type: GrantFiled: February 21, 1990Date of Patent: May 7, 1991Assignee: American Cyanamid CompanyInventors: Shin S. Tseng, Joseph W. Epstein, Jeremy I. Levin
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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: 4992442Abstract: Pyrrolo[3,2-e]pyrazolo[1,5-a]pyrimidine derivatives are disclosed. The compounds are represented by the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 individually represent a hydrogen atom, a linear or branched alkyl group which may have a substituent, a cycloalkyl or phenyl group which may have a substituent, or a heterocyclic group which may have a substituent, and R.sub.3 is a hydrogen atom or a cyano group. The compounds have excellent circulatory disease curing activities as well as bronchodilation activities.Type: GrantFiled: October 3, 1989Date of Patent: February 12, 1991Assignee: Pola Chemical Industries Inc., JapanInventors: Michihiko Tsujitani, Kenichi Kishii, Masato Inazu, Toshihiro Morimoto, Yoshiaki Motoki, Ichiro Matsuo
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Patent number: 4977190Abstract: Riboflavin produced by a microbial method is prepared in the form of free-flowing, non-dusting, spray-dried granules or microgranules as a feed additive by removing water from the mixture discharged from microbial fermentation for the preparation of riboflavin, wherein the mixture is subjected to(a) a fluidized-bed spray-drying process(b) a one-material spray-drying process or(c) a disk spray-drying process without significant amounts of binders being added to the discharged fermentation mixture.Type: GrantFiled: June 9, 1989Date of Patent: December 11, 1990Assignee: BASF AktiengesellschaftInventors: Joachim Meyer, Wolfgang Buehler, Johannes Grimmer, Gunter Eipper, Hans Kiefer, Christoph Martin
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Patent number: 4968690Abstract: The new compound 3-deazaneplanocin A has been discovered to have potent anti-viral, anti-tumor activity and differentiating activity. A simple method for preparing 3-deazaneplanocin A has been developed involving nucleophilic substitution, which method can also be used to prepare a great variety of carbocyclic nucleosides.Type: GrantFiled: January 19, 1989Date of Patent: November 6, 1990Assignee: United States Government as represented by the Secretary of the Dept. of Health and Human ServicesInventors: Victor E. Marquez, John S. Driscoll, Mu-Ill Lim, Christopher K. Tseng, Alberto Haces, Robert I. Glazer
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Patent number: 4968797Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicalsX.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 30, 1987Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
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Patent number: 4954498Abstract: The present invention provides tricyclic benzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or diferent as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.Type: GrantFiled: January 15, 1988Date of Patent: September 4, 1990Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Erwin Boehm, Klaus Strein
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Patent number: 4925939Abstract: The present invention concerns compounds of the formula: ##STR1## wherein R is a lower alkyl group, an aryl group or an alkylaryl group and X and Y are the same or different, and each is OH, NH.sub.2, or SH. The aryl group or the aryl moiety of the alkylaryl group may be unsubstituted, monosubstituted, disubstituted or trisubstituted. If substituted, each substituent may independently be an alkyl group, an alkyloxy group or a halogen.The present invention also provides methods for synthesizing the compounds described above.Type: GrantFiled: January 5, 1989Date of Patent: May 15, 1990Assignee: Sloan-Kettering Institute for Cancer ResearchInventor: Kyoichi A. Watanabe
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Patent number: 4916137Abstract: This disclosure described novel 5-(substituted-amino)-8-(substituted-phenyl)-3H,6H, -1,-4,5a,8a-tetraazaacenaphthylen-3-ones useful for the treatment of cognitive and related neural behavioral disorders in mammals.Type: GrantFiled: November 30, 1988Date of Patent: April 10, 1990Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Jeremy I. Levin, Shin S. Tseng
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Patent number: 4912104Abstract: Novel tricyclic fused pyrimidine derivatives represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently C.sub.1-8 alkyl or C.sub.2-8 alkenyl;R.sup.3 is hydrogen, C.sub.1-3 alkyl, C.sub.2-3 alkenyl, C.sub.1-6 alkyl-CO-, optionally substituted benzoyl, C.sub.1-4 alkyl-O-CO-, carbamoyl or formyl; andA is C.sub.2-4 alkylene or C.sub.2-4 alkenylene which may be substituted with C.sub.1-3 alkyl, halogen, nitro, amino, oxo, or phenyl optionally substituted with 1 to 2 members selected from the class consisting of amino, nitro, hydroxy, methoxy and methyl, and a salt thereofare useful for antiinflammatory, analgesic, antipyretic, anti-allergic anti-psoriatic and liver-protecting agent.Type: GrantFiled: August 16, 1988Date of Patent: March 27, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Takehiko Naka, Taketoshi Saijo, Hiroshi Satoh
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Patent number: 4904658Abstract: Substituted-6H,8H-pyrimido[1,2,3-cd]purine-8,10(9H)-diones and substituted-6H,10H-pyrimido[1,2-cd]purin-10-ones which are useful as cognition enhancing agents, anxiolytic agents and/or antihypertensive agents in the treatment of cognitive and relative neutral behavioral problems, anxiety and hypertension in mammals.Type: GrantFiled: April 15, 1988Date of Patent: February 27, 1990Assignee: American Cyanamid CompanyInventors: Shin S. Tseng, Joseph W. Epstein, Jeremy I. Levin
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Patent number: 4902686Abstract: New heterocyclic compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## CO.sub.2 R' or CONR'R", wherein R' and R" independently are C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;--A-- is --C(.dbd.O)--NR'"--, --NR'"--C(.dbd.O)--, or ##STR3## wherein R'" is C.sub.1-6 -alkyl; X is C or N; andR.sup.4 is hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.1-6 -alkynyl, trimethylsilyl-C.sub.1-6 -alkynyl, aryloxy which may be substituted with halogen, aralkoxy, C.sub.3-7 -cycloalkoxy which may be substituted with one or more C.sub.1-6 -alkyl groups, or NR""R'"", wherein R"" and R""' independently are C.sub.1-6 -alkyl or together with the nitrogen atom form a 3-7 membered heterocyclic ring.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.Type: GrantFiled: April 20, 1989Date of Patent: February 20, 1990Assignee: A/S FerrosanInventors: Frank Watjen, Holger C. Hansen
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Photopolymerizable composition containing salts of organic cationic dyes and organic boron compounds
Patent number: 4902604Abstract: Photopolymerizable initiator compositions having high photosensitivity to light sources giving visible rays and the other rays in the longer wavelengths. The compositions containing polymerizable compounds having ethylenic unsaturated bonds and salts formed by an organic boron compound anion and an organic cationic azulene dye compound comprising an azulene ring having a nitrogen atom or a chalcogen atom in the 2- or 4- position can be used for making lithographic printing plates, resinous relief printing plates, and resists or photomasks for printed circuit substrates.The polymerizable compounds having ethylenic unsaturated bonds can be encapsulated to obtain microcapsules to be used for the formation of black-and-white or color images.Type: GrantFiled: September 30, 1988Date of Patent: February 20, 1990Assignee: Fuji Photo Film Co., Ltd.Inventors: Jun Yamaguchi, Masaki Okazaki, Takanori Hioki -
Patent number: 4900819Abstract: The disclosure relates to a method of initiating a crystal growth prior to filtering off, from the mother liquor in which they were produced, of such crystalline explosives of the type hexogen and octogen produced by the so-called Bachmann process or variations of this process.According to the invention, the mother liquor is, after the end of the chemical reaction proper, subjected to a pressure-heat treatment which initiates the partial dissolution of the crystalline explosives obtained in the process, giving rise, after cooling of the mother liquor, to larger crystals which may more readily be filtered off.According to a further improvement of the invention a relatively pure octogen may be extracted from the mother liquor by way of a thermo-filtering of said liquor at a temperature of 60.degree.-110.degree. C.Type: GrantFiled: April 21, 1988Date of Patent: February 13, 1990Assignee: Nobel Kemi ABInventors: Per Ericsson, Leif Svensson, Nils-Ingvar Olsson, Bertil Bergstrom
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Patent number: 4898943Abstract: Novel tricyclic triazolopyrimidine compounds represented by formula (I) shown in the specification and physiologically acceptable salts thereof are disclosed. These compounds have an excellent anti-allergic activity and are useful for treatment and prophylaxis of allergic diseases.Type: GrantFiled: February 8, 1988Date of Patent: February 6, 1990Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Sumiro Isoda, Shunzo Aibara, Tamotsu Miwa, Hiroyuki Fujiwara, Shuichi Yokohama, Hiroo Matsumoto
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Patent number: 4873244Abstract: New heterocyclic compounds having the general formula ##STR1## wherein ##STR2## CO.sub.2 R' or CONR'R", whereinR' and R" independently are C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;--A-- is --C(.dbd.O)--NR'"--, --NR'"--C(.dbd.O)--, or ##STR3## wherein R'" is C.sub.1-6 -alkyl;X is C or N; andR.sup.4 is hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.1-6 -alkynyl, trimethylsilyl-C.sub.1-6 -alkynyl, aryloxy which may be substituted with halogen, aralkoxy, C.sub.3-7 -cycloalkoxy which may be substituted with one or more C.sub.1-6 -alkyl groups, or NR""R'"", wherein R"" and R'"" independently are C.sub.1-6 -alkoxy or together with the nitrogen atom form a 3-7 membered heterocyclic ring.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.Type: GrantFiled: February 16, 1988Date of Patent: October 10, 1989Assignee: A/S FerrosanInventors: WaFrank, Holger C. Hansen
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Patent number: 4871732Abstract: The present invention is directed to a group of compounds which are imidazo[2,1-b]quinazolin-5(3H)-ones, related tricyclic compounds, and pharmaceutically acceptable salts thereof. These compounds are useful as bronchodilators. These compounds are prepared by the reaction of an appropriate hydrazine with an appropriate 1-substituted-2-methyl-2-imidazoline or chemically equivalent compound.Type: GrantFiled: September 22, 1988Date of Patent: October 3, 1989Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, Shyam Sunder
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Patent number: 4859774Abstract: The flowability of stored triethylenediamine is improved by admixing with a flow promoting amount of a salt, amide or ester derivative of a C.sub.8 -C.sub.22 fatty acid. Especially suitable flow promoting additives for triethylenediamine are sales of stearic acid.Type: GrantFiled: April 14, 1988Date of Patent: August 22, 1989Assignee: Air Products and Chemicals Inc.Inventors: Akio Takahashi, Robert G. Petrella, Joel Schwartz
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Patent number: 4847377Abstract: Substituted 2,3-dihydro-6-substituted-pyrimido[2,1-f]purine-4,8(1H, 9H)-diones, their tautomers and salts, are disclosed for use as antihyperproliferative skin disease agents.Methods for their preparation and use are described.Type: GrantFiled: October 8, 1987Date of Patent: July 11, 1989Assignee: Schering CorporationInventors: Daniel M. Solomon, James J. Kaminski, David J. Conn
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4831013Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, or ribofuranosyl; X is oxygen, NR, or sulfur; R is hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and ring A is (a) an optionally substituted 5-8 membered monocycloalken-1,2-diyl; (b) an optionally substituted carbobicyclic ring of the formula ##STR2## wherein n and m are each independently one or two; or (c) an optionally substituted 5-6 membered heterocycle having one or two heteroatoms, the atoms of which are selected from carbon, oxygen, nitrogen, and sulfur. Also disclosed are tautomers of the above and pharmaceutically acceptable salts; compositions thereof; and methods of using the compounds, tautomer, or salts.Type: GrantFiled: February 27, 1987Date of Patent: May 16, 1989Assignee: Ciba-Geigy CorporationInventor: John E. Francis
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Patent number: 4831029Abstract: The invention relates to condensed cyclic triazole derivatives of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof. The compounds of the general Formula I possess useful sedative and tranquillant properties and exhibit particularly spasmolytic, motility inhibiting, and narcosis potentiating, yohimbine potentiating and local anaesthetic and also weak reserpine ptosis inhibiting effect.Type: GrantFiled: November 5, 1987Date of Patent: May 16, 1989Inventors: Jozsef Reiter, Endre Rivo, Klara Reiter nee Esess, Marton Fekete, Frigyes Gogenyi, Lujza Petocz, Istvan Gacsalyi, Istvan Gyertyan
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Patent number: 4826981Abstract: There is disclosed a process for preparing 9-(2-hydroxyethoxymethyl)-guanine (acyclovir) of the formula IV ##STR1## wherein a novel compound of the formula I ##STR2## wherein R and R' may be the same or different and represent hydrogen, (C.sub.1 -C.sub.8)acyl or benzyl and R.sub.1 represents (C.sub.1 -C.sub.8)acyl, is hydrolyzed basic conditions. Also disclosed is the novel compound of the formula I, a process for the preparation thereof by condensing a novel compound of the formula II ##STR3## with a compound A--CH.sub.2 --O--CH.sub.2 CH.sub.Type: GrantFiled: October 19, 1987Date of Patent: May 2, 1989Assignee: KRKAInventors: Joze Kobe, Joze Gnidovec, Pavle Zupet
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Patent number: 4816458Abstract: Substituted 2,3-dihydro-6-substituted-pyrimido[2,1-f]purine-4,8(1H,9H)-diones, their tautomers and salts, are disclosed for use as antihyperproliferative skin disease agents.Methods for their preparation and use are described.Type: GrantFiled: December 19, 1986Date of Patent: March 28, 1989Assignee: Schering CorporationInventors: Daniel M. Solomon, James J. Kaminski
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Patent number: 4806643Abstract: Riboflavin of the formula I ##STR1## is prepared by an improved process by condensing a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline of the formula II ##STR2## where R is H, --CL, --NO.sub.2, --CH.sub.3 or --OCH.sub.3 in the o- or p-position, with barbituric acid of the formula III ##STR3## in the presence of an acid as a condensing agent, by a process in which the acidic condensing agent used is an aliphatic secondary carboxylic acid of the general formula IV ##STR4## where R.sup.1 is methyl or ethyl and R.sup.2 is alkyl of 3 or 4 carbon atoms.Type: GrantFiled: November 19, 1986Date of Patent: February 21, 1989Assignee: BASF AktiengesellschaftInventor: Johannes Grimmer
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Patent number: 4778511Abstract: Novel fluorine-containing N-sulfenylated indazoles are prepared by reacting the corresponding indazoles with sulfenyl halides in the presence of a solvent and/or diluent and in the presence of an acid-binder. The novel fluorine-containing N-sulfenylated indazoles are useful in the protection of industrial materials against attack by microorganisms such as bacteria, fungi, yeast, algae, and slime as plant protection agents, and in combating insects and arachrids.Type: GrantFiled: February 18, 1986Date of Patent: October 18, 1988Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Bernd Baasner, Albrecht Marhold, Wilfried Paulus, Paul Reinecke, Hans-Georg Schmitt
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Patent number: 4754034Abstract: 4,4-diaryldihydroquinazolones of the formula ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3, independently of one another, denote hydrogen, halogen, alkyl, aryl, alkanoylamino, aroylamino, heteryl, NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3, at least one of the radicals X.sup.1, X.sup.2 or X.sup.3 standing for NY.sup.1 Y.sup.2, OY.sup.3 or SY.sup.3,R.sup.1 denotes hydrogen, alkyl, cycloalkyl, aralkyl, aryl or the members of a bridge to the o-carbon of ring C,R.sup.2 denotes a radical of an acid,Y.sup.1, Y.sup.2 and Y.sup.3, independently of one another, denote hydrogen, alkyl, cycloalkyl, aralkyl aryl or heteryl or the remaining members of a 5- or 6-membered ring which reaches to one of the o-position benzene C atoms and may contain further hetero atoms orY.sup.1 +Y.sup.Type: GrantFiled: October 21, 1985Date of Patent: June 28, 1988Assignee: Bayer AktiengesellschaftInventors: Horst Berneth, Alfred Brack, Karlheinrich Meisel
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Patent number: 4725596Abstract: Certain pyrimidine derivatives are useful in treating allergic, inflammatory and hyperproliferative skin diseases and in suppressing the immune response. Methods for preparing the compounds and methods for their use are also described.Type: GrantFiled: August 15, 1986Date of Patent: February 16, 1988Assignee: Schering CorporationInventors: Richard J. Friary, Sidney R. Smith, Marvin I. Siegel
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Patent number: 4716161Abstract: A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention.Type: GrantFiled: April 3, 1985Date of Patent: December 29, 1987Assignee: Mitsubishi Chemical Industries LimitedInventors: Harukazu Fukami, Ryoji Kikumoto, Kenichiro Nakao, Issei Nitta, Shinya Inoue