Barbituric Acid Or Derivative (including Thioanalogs) Patents (Class 514/270)
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Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5614541Abstract: New catechol derivatives and pharmaceutically acceptable salts and esters thereof useful as pharmaceutical antioxidants are disclosed. Cellular damage by oxygen derived radicals is a significant factor in heart disease, rheumatoid arthritis, cancer, inflammatory disease, transplant rejection reactions and ischemia.Type: GrantFiled: October 18, 1994Date of Patent: March 25, 1997Assignee: Orion-yhtym a OyInventors: Reijo B ackstr om, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 5543147Abstract: A crystalline modification of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine prepared by cooling a solution of 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine in water, an organic solvent or in a mixture thereof with a cooling agent at a rate not below 6.degree. C./min to crystallization followed by separation of the obtained crystals and drying them. The crystalline modification has high antiinflammatory and wound-healing activity and is an active substance in medicaments used for treatment of burns and wounds of various organs.Type: GrantFiled: November 17, 1994Date of Patent: August 6, 1996Assignee: Nikolai B. LeonidovInventors: Nikolai B. Leonidov, Nikolai G. Selezenev
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Patent number: 5489590Abstract: A therapeutic composition derived from a pre-activated photoactive compound and a conveyor for destroying tumor or other pathogenic biological contaminants infecting animal body tissues. The conveyor can either be a matrix support or an antibody. The activation of the photoactive compound to produce the pre-activated photoactive compound is carried out by the use of an activating agent. The pre-activated photoactive compound retains its therapeutic activity subsequent to activation. A method for preparing such a therapeutic composition is disclosed. Methods for treating animal body tissue, either outside the body or inside the body, infected with tumors or other pathogenic biological contaminants are disclosed.Type: GrantFiled: February 3, 1992Date of Patent: February 6, 1996Assignee: Baylor Research FoundationInventors: Kirpal S. Gulliya, Shazib Pervaiz, J. Lester Matthews, Robert M. Dowben, Jospeh T. Newman, Edward Forest
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Patent number: 5476855Abstract: Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging.Type: GrantFiled: November 2, 1993Date of Patent: December 19, 1995Assignees: Mahmoud H. el Kouni, Fardos N. M. Naguib, F. SchinaziInventors: Mahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
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Patent number: 5474990Abstract: Certain barbiturates have been shown to completely prevent the neurotoxic injury to cerebrocortical neurons that can be caused by NMDA antagonists. The use of barbiturates as "safening agents" allows NMDA antagonists (including powerful NMDA antagonists such as MK-801) to be used safely as neuroprotectants to prevent brain damage due to hypoxia/ischemia caused by strokes, cardiac arrest, perinatal asphyxia, and various other conditions.Type: GrantFiled: July 22, 1991Date of Patent: December 12, 1995Inventor: John W. Olney
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Patent number: 5474996Abstract: Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.Type: GrantFiled: May 22, 1992Date of Patent: December 12, 1995Assignee: Roussel UclafInventors: Jean-Claude Caille, Stanislas Didierlaurent, Jean-Paul Vevert
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Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
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Patent number: 5362733Abstract: Compounds of formula(I) ##STR1## wherein R.sub.1 is nitro, halo, cyano and R.sub.2 is a group selected from ##STR2## wherein Y is oxygen or sulfur; X.sub.1 is NR wherein R is hydrogen, C.sub.1-8 alkyl or phenyl and pharmaceutically acceptable salts thereof are useful in the prevention or treatment of tissue damage induced by lipid peroxidation.Type: GrantFiled: October 23, 1992Date of Patent: November 8, 1994Assignee: Orion-yhtyma OyInventors: Reijo Backstrom, Erkki Honkanen, Inge-Britt Linden, Erkki Nissinen, Aino Pippuri, Pentti Pohto, Tapio Korkolainen
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Patent number: 5278167Abstract: Novel 6-pyridyl substituted pyrimidine derivatives are disclosed for use as antiviral agents, particularly for the treatment of retroviral infections such as HIV infections and related disorders, as well as for use in anti-cancer therapies to improve the efficacy of anti-cancer therapeutics. These compounds and their pharmacologically acceptable salts operate to disrupt viral replication an exhibit lower cell toxicity, thereby providing more efficient agents for use alone or in conjunction with other chemical or biological agents to provide prolonged antiviral therapy. In addition, the compounds can be used to increase the efficacy of anti-cancer therapeutics including 5-fluropyrimidines such as 5-fluorouracil, thereby reducing the dosage requirement of the therapeutic in anti-cancer therapies so as to decrease toxic effects to the host.Type: GrantFiled: May 13, 1992Date of Patent: January 11, 1994Assignee: Brown University Research FoundationInventors: Shih H. Chu, Yung C. Cheng, Bai C. Pan
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Patent number: 5262402Abstract: This invention relates to a process for preparation of pyrimidinetriones. It also relates to novel N-dihydroxyphosphoryl pyrimidinetrione derivatives which may be useful as water-soluble prodrugs of certain pyrimidinetrione compounds.Type: GrantFiled: October 30, 1991Date of Patent: November 16, 1993Assignee: Sapos S.A.Inventors: Bernard Siegfried, Jindrich Vachta, Karel Valter, Stephane Hugentobler
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Patent number: 5252577Abstract: A method of desensitizing a hypersensitive tooth by topically applying to the tooth a composition including an amount of a barbiturate effective to desensitize the tooth. This desensitizing composition may be included in an excipient or in a sustained-release matrix or microbeads that can be incorporated into toothbrushes, dental floss, dentifrices, dental rinses, etc.Type: GrantFiled: March 6, 1992Date of Patent: October 12, 1993Assignee: Gillette Canada, Inc.Inventors: Miklos M. Breuer, Samuel S. Turesky
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Patent number: 5250536Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5- or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; are useful as nematicides.Type: GrantFiled: March 18, 1992Date of Patent: October 5, 1993Assignee: Imperial Chemical Industries PLCInventor: Michael D. Turnbull
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Patent number: 5248683Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.Type: GrantFiled: June 4, 1992Date of Patent: September 28, 1993Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Walter Kunz, Rolf Schurter
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Patent number: 5246938Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5 - or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; provided that when n is 0, R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen, or when n is 0 and R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are not both methyl, or when n is 0 and R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 is not methyl; are useful as nematicides.Type: GrantFiled: March 18, 1992Date of Patent: September 21, 1993Assignee: Imperial Chemical Industries PLCInventors: Michael D. Turnbull, John Finney
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Patent number: 5234923Abstract: Novel compounds are disclosed having the formula ##STR1## or its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: December 16, 1991Date of Patent: August 10, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Michael A. Poss, Karnail S. Atwal
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Patent number: 5234929Abstract: A method of treating or preventing motion sickness is disclosed which comprises administering an anti-motion sickness effective amount of an anticonvulsant compound such as phenytoin, ethotoin, primidone, ethosuximide or carbamazepine, in combination with a potentiating amount of an antitussive or cough suppressant agent such as dextromethorphan, levopropoxyphene, muscaphene, pholocodeine, or carbetapentene. The antitussive compounds of the present invention act as potentiating agents so as to enable effective treatment or prevention of motion sickness using a reduced amount of the anticonvulsant compound normally used in such treatment. The method of the present invention reduces the potential for various side effects and thus provides a safer and more effective method of treatment for motion sickness than prior art methods.Type: GrantFiled: July 20, 1992Date of Patent: August 10, 1993Inventor: William Chelen
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Patent number: 5204354Abstract: Substituted quinazolinones of the formula are useful as neurotensin antagonists.Type: GrantFiled: February 14, 1992Date of Patent: April 20, 1993Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, E. M. Naylor, Richard W. Ransom
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Patent number: 5202329Abstract: Pyrimidinyloxy(thio)quinoline derivatives represented by the formula (I) which exhibit an excellent controlling effect for plant diseases and are also safe for crop plants, preparation processes of the derivatives, and agri-horticultural fungicides comprising the derivatives as an active ingredient, are disclosed. ##STR1## In the formula (I), X is an oxygen atom or sulfur atom, Y is a hydrogen atom or halogen atom, Z is a hydrogen atom or methyl, R.sup.1 and R.sup.2 are methoxy or methyl, and n is an integer of 1 or 2.Type: GrantFiled: March 11, 1992Date of Patent: April 13, 1993Assignee: Mitsui Toatsu Chemicals Inc.Inventors: Katsutoshi Ishikawa, Yukihiro Yoshikawa, Tsutomu Ishii, Hiroharu Tanikawa, Sunao Maeda, Hideo Kawashima, Yuji Yanese, Hitoshi Shimotori, Ryuichi Mita
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Patent number: 5166207Abstract: A method for enhancing the systemic delivery of dextromethorphan for the treatment of a neurological disorder resulting in injury to nervous tissue, which comprises administering to a patient suffering from the disorder an amount of a cytochrome P450IID6 enzyme inhibitor, sufficient to block dextromethorphan metabolism, and an amount of dextromethorphan sufficient to treat the neurological disorder. Quinidine is particularly suitable for use in the method of the invention.Type: GrantFiled: June 17, 1991Date of Patent: November 24, 1992Assignee: NeuroTherapeutics, Inc.Inventor: Richard A. Smith
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Patent number: 5164416Abstract: A transdermal therapeutic formulation comprising d-limonene and at least one pharmaceutically active substance wherein the content of the d-limonene is in the range from 0.1 to 2 weight percent, based on the total amount of the formulation. The transdermal therapeutic formulation has an excellent percutaneous absorption, is safe and is capable of delivering desired pharmaceutically active substances to a desired location of treatment or to the entire body of a patient through the circulatory system and is thus effective for curing various diseases.Type: GrantFiled: May 8, 1991Date of Patent: November 17, 1992Assignee: Lintec CorporationInventors: Tsuneji Nagai, Kozo Takayama, Hideaki Okabe
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Patent number: 5164396Abstract: The invention relates to new barbituric acid derivatives of the general formula ##STR1## wherein R is a substituted or unsubstituted phenyl group or heteroaryl group having 5 or 6 ring atoms, the heteroaryl group comprising one or more hetero atoms selected from the group consisting of N, O and S, and the substituents being selected from the group consisting of halogen, cyano, nitro, formyl, acetyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy and optionally substituted phenoxy;R.sub.1 is a C.sub.3 -C.sub.5 alkyl group, a C.sub.3 -C.sub.5 alkenyl group, a C.sub.3 -C.sub.5 alkynyl group, a cyclopropyl group or a cyclopropyl(C.sub.1 -C.sub.4)alkyl group, andR.sub.2 is a C.sub.1 -C.sub.4 alkyl group or an amino group;as well as salts and metal complexes of the said compounds.These compounds may be used in compositions for the control of insects, in particular aphids, in agriculture, horticulture and silviculture.Type: GrantFiled: May 1, 1991Date of Patent: November 17, 1992Assignee: Duphar International Research B.V.Inventors: Arnoldus C. Grosscurt, Jan W. Terpstra
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Patent number: 5162327Abstract: Pyrimidinetrione derivatives, processes for their preparation, agents containing them and their use as agents for combating pests.Compounds of the formula I, tautomeric forms thereof of the formula Ia, stereoisomers thereof and the mixtures of these forms ##STR1## wherein R.sup.1 and R.sup.2 denote unsubstituted or substituted alkyl, alkenyl, alkynyl; alkoxy, alkylsulfonyl, alkylcarbonyl or cyano or optionally substituted phenyl, phenylsulfonyl or phenylcarbonyl,R.sup.3 denotes hydrogen, alkyl or optionally substituted phenyl,R.sup.4 denote H, OH, unsubstituted or substituted alkyl, alkenyl, alkynyl, phenylsulfonyl, phenylcarbonyl, phenylcarbamoyl or phenyl; alkylsulfonyl or alkylcarbonyl, which can be halogenated, alkylcarbamoyl or cyano,R.sup.5 and R.sup.Type: GrantFiled: February 2, 1990Date of Patent: November 10, 1992Assignee: Hoechst AktiengesellschaftInventors: Gunter Kratt, Gerhard Salbeck, Werner Bonin, Dieter Duwel
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Patent number: 5141943Abstract: 5-benzyl barbiturate compounds for use as water-soluble uridine phosphorylase inhibitors are disclosed. These compounds are useful for reducing the toxicity and anemia induced by antiviral drugs such as AZT, as well as for potentiating anticancer drugs and combatting their host-toxicity.Type: GrantFiled: April 12, 1990Date of Patent: August 25, 1992Assignee: Brown University Research FoundationInventors: Fardos N. M. Naguib, Mahmoud H. el Kouni, Raymond Panzica, Sungman Cha
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Patent number: 5130317Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.Type: GrantFiled: September 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
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Patent number: 5130412Abstract: An electrically conducting self-doped carbazole polymer of the formula: ##STR1## wherein A is a bifunctional molecule capable of bonding to a positively charged molecule at one end and is capable of bonding to a flexible spacer group Z at another end, Z is a flexible spacer group capable of bonding to an anionic group A at one end and is capable of bonding either to a nitrogen or aromatic electron withdrawing or electron donating group at another end, E is a bifunctional molecule capable of bonding to nitrogen at one end and is capable of bonding to a flexible spacer group Z at anther end, X is a positively charged counterion, and n is at least 2.Type: GrantFiled: October 16, 1990Date of Patent: July 14, 1992Assignee: Southwest Research InstituteInventors: Stephen T. Wellinghoff, Charles K. Baker
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Patent number: 5108733Abstract: Spontaneous aspecific coloration in so-called Trinder reagents which can alter subsequent colorimetric determinations is inhibited by adding compounds of the chelating agent class to the solution. The resultant compositions contain a peroxidase enzyme, a phenylpyrazone derivative, a compound of phenolic or aromatic amine structure and a stabilizer. Preferred stabilizers are ethylenediaminetetraacetic acid (EDTA) and diethylenetriaminepentaacetic acid (DTPA).Type: GrantFiled: August 30, 1990Date of Patent: April 28, 1992Assignees: Instrumentation Laboratory S.p.A., 501 Instrumentation Laboratory S.p.A.Inventors: Dario Frontini, Maurizio D'Alterio
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Patent number: 5109004Abstract: A phenyl substituted heterocyclic compound of formula (I): ##STR1## wherein R.sup.1 is optionally substituted pyridone, thiopyridone, pyrimidinthione, pyrimidinone, pyrazole, imidazole or triazole group; R.sup.2 is hydrogen, halogen, haloalkyl, nitro or cyano; R.sup.3 and R.sup.5 are independently selected from hydrogen, halogen, alkyl or cycloalkyl; R.sup.4 is halogen, haloalkyl, haloalkoxy or S(O).sub.n R.sup.6 where R.sup.6 is alkyl, haloalkyl or cycloalkyl and n is 0, 1 or 2; having insecticidal activity.Type: GrantFiled: April 10, 1990Date of Patent: April 28, 1992Assignee: Imperial Chemical Industries PLCInventors: Nicola J. Bettesworth, Maureen Smith, Trevor R. Perrior, Alan J. Whittle, Alfred G. Williams, Donn W. Moseley
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Patent number: 5091385Abstract: A pre-activated therapeutic agent derived from a photoactive compound for destroying tumor or other pathogenic biological contaminants infecting animal body tissues. The activation of the photoactive compound is carried out prior to the photoactive compound is being brought into contact with the tissue to be treated. The resultant pre-activated therapeutic agent, or mixture, retains its therapeutic activity subsequent to activation. A method for preparing such a pre-activated therapeutic agent is disclosed. Methods for treating animal body tissue, either outside the body or inside the body, infected with tumors or other pathogenic biological contaminants are disclosed.Type: GrantFiled: September 30, 1988Date of Patent: February 25, 1992Assignee: Baylor Research InstituteInventors: Kirpal S. Gulliya, Shazib Pervaiz, J. Lester Matthews, Robert M. Dowben, Joseph T. Newman, Edward Forest
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Patent number: 5081125Abstract: Anthelmintically active compounds of formula I are described ##STR1## in which R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 thioalkyl, C.sub.1 -C.sub.2 haloalkyl, nitro, C.sub.1 -C.sub.2 alkoxy, or the group SO.sub.n R in which R is C.sub.1 -C.sub.2 alkyl or phenyl and n is 0, 1 or 2;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.3 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.6 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.7 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, nitro, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.8 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.9 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.Type: GrantFiled: September 19, 1990Date of Patent: January 14, 1992Assignee: Ciba-Geigy CorporationInventors: Peter Maienfisch, Christor Hildenbrand, Jean-Claude Gehret
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Patent number: 5081142Abstract: Compounds of the formula I ##STR1## where Ar is unsubstituted or substituted phenyl, pyridyl, thienyl or napthyl,R.sup.1 is hydrogen or CN,R.sup.2 is unsubstituted or substituted aryl, hetaryl, alkyl or cycloalkyl, or is unsubstituted or substituted alkenyl or alkynyl,x is CH.sub.2, O or S andn is 0 or 1,their plant-tolerated acid addition salts and metal complexes, and fungicides and growth regulators containing these compounds.Type: GrantFiled: September 28, 1990Date of Patent: January 14, 1992Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Thomas Zierke, Wolfgang Reuther, Ulf Baus, Gisela Lorenz, Eberhard Ammermann
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Patent number: 4994465Abstract: Certain trisubstituted urea compounds as potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase, their method of manufacture, pharmaceutical compositions containing such compounds as well as methods of inhibiting the interstitial absorption of cholesterol and lowering blood plasma cholesterol with such compounds as described.Type: GrantFiled: February 5, 1990Date of Patent: February 19, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4992443Abstract: Certain anticonvulsant drugs have been found to be effective in the treatment of motion sickness. These compounds have the structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are H, aliphatic or aromatic groups;B is --C.dbd.O or --CH.sub.2 --;n' is 0 or 1;n" is 0 or 1; andX is ##STR2## with the further proviso that when n' is 1, n" is also 1, and their non-toxic, pharmaceutically acceptable acid addition salts.Type: GrantFiled: March 12, 1990Date of Patent: February 12, 1991Inventor: William Chelen
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Patent number: 4942155Abstract: The novel compounds are provided with good antibacterial and antitumour activity.Type: GrantFiled: March 9, 1987Date of Patent: July 17, 1990Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Giuseppe Cassinelli, Arpad Grein, Sergio Merli, Giovanni Rivola
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Patent number: 4880811Abstract: The present invention provides a method for decreasing the bodily content of uric acid in a subject which comprises administrating to the subject an effective content-decreasing amount of a barbiturate compound mono-substituted at the carbon-5 position.The invention also provides a pharmaceutical composition and a method for treating disorders of uric acid metabolism and resulting ailments in a subject.Type: GrantFiled: June 24, 1987Date of Patent: November 14, 1989Assignee: Memorial Hospital for Cancer and Allied DiseasesInventor: Raymond P. Warrell, Jr.
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Patent number: 4879276Abstract: Method for reducing uric acid levels in mammals, comprising administering compounds having the formula: ##STR1## wherein A is selected from the group consisting of ##STR2## and --CH.sub.2 --; X is oxygen or sulfur; R.sub.6 is hydrogen, an alkoxy group having from one to four carbon atoms, or alkylthio, amino, dialkylamino, or NHR.sub.7 wherein R.sub.7 is alkyl, aryl or arylamino, the alkyl moieties of which have from 1 to 12 carbon atoms;R.sub.1 and R.sub.2 may each independently be hydrogen; alkyl, aryl, aralkyl, aralkenyl or aralkynyl, the alkyl, alkenyl or alkynyl moieties of which have from one to six carbon atoms, or a carbohydrate residue;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or aryl;R.sub.Type: GrantFiled: January 11, 1988Date of Patent: November 7, 1989Assignee: Uniroyal Chemical Ltd./Uniroyal Chemical LteeInventor: Arthur D. Brewer
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Patent number: 4879274Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.Type: GrantFiled: September 12, 1986Date of Patent: November 7, 1989Assignee: Kao CorporationInventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
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Patent number: 4833148Abstract: Methods and compositions are described for treatment to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an alkenyl-substituted or alkynyl-substituted thiobarbiturate characterized in having broad-spectrum activity as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.Type: GrantFiled: April 9, 1987Date of Patent: May 23, 1989Assignee: Washington UniversityInventor: John W. Olney
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Patent number: 4824850Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D--DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.Type: GrantFiled: October 29, 1984Date of Patent: April 25, 1989Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4816460Abstract: 1,3-Dimethyl-4,6-dioxo-2-thioxo-N-[4-(4'trifluoromethylphenoxy)phenyl] perhydropyrimidine-5-carboxamide and analogues are useful pesticides, particularly against insect pests of timber.Type: GrantFiled: December 9, 1986Date of Patent: March 28, 1989Assignee: Burroughs Wellcome Co.Inventor: John P. Larkin
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Patent number: 4762830Abstract: The invention relates to novel 5-(azolyloxyphenylcarbamoyl)barbituric acid derivatives of the general formula I ##STR1## wherein X is oxygen or sulfur;R.sub.1 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 cycloalkyl or allyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl or allyl;R.sub.3 is an unsubstituted or substituted five-membered azole ring which is bound through carbon and is selected from the group consisting of benzimadazole, benzoxazole, benzothiazole, imidazole, oxazole, thiazole, oxadiazole, thiadiazole and triazole; andR.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 haloalkoxy;and to the tautomers and salts thereof, as anthelmintic compounds. Together with suitable carriers and further assistants, these compounds may be used in particular for controlling helminths which are parasites of animals.Type: GrantFiled: February 13, 1986Date of Patent: August 9, 1988Assignee: Ciba-Geigy CorporationInventors: Elmar Sturm, Jean J. Gallay, Haukur Kristinsson, Georg Pissiotas
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Patent number: 4748178Abstract: Novel phenylcarbamoylbarbituric acid derivatives of the general formula I ##STR1## and tautomeric forms and salts thereof in which R.sub.1 and R.sub.2 independently of one another are C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.3 -alkoxy, C.sub.3 -C.sub.6 -cycloalkyl, allyl or phenyl; R.sub.3 is substituted or unsubstituted pyridyl as herein defined; and X is oxygen or sulfur; they possess anthelmintic activity. The active substances can be employed in conjunction with suitable carriers and further adjuncts for controlling zooparasitic helminths.Type: GrantFiled: February 13, 1986Date of Patent: May 31, 1988Assignee: Ciba-Geigy CorporationInventors: Urs Burckhardt, Jean J. Gallay, Manfred Kuhne
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Patent number: 4670441Abstract: The invention relates to novel 5-phenylcarbamoylthiobarbituric acid derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently C.sub.1 -C.sub.5 alkyl or methoxy,R.sub.3 is unsubstituted phenyl, unsubstituted pyridyl, or phenyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 cyanoalkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms, or is pyridyl which is substituted by 1 to 3 identical or different members selected from the group consisting of C.sub.1 -C.sub.5 alkyl, halogen, nitro and C.sub.1 -C.sub.5 haloalkyl containing 1 to 5 halogen atoms andR.sub.4 and R.sub.5 are each independently hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.2 haloalkyl containing 1 to 3 halogen atoms, or are C.sub.1 -C.sub.3 -alkoxy or nitro,and to the tautomers and salts thereof, as anthelmintics.Type: GrantFiled: July 5, 1985Date of Patent: June 2, 1987Assignee: Ciba-Geigy CorporationInventors: Manfred Kuhne, Jean J. Gallay
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Patent number: 4666913Abstract: A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.Type: GrantFiled: November 22, 1985Date of Patent: May 19, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kubla, Henry F. Campbell, William L. Studt, Bruce F. Molino, Thomas J. Tucker
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Patent number: 4661478Abstract: There is disclosed a process for treating a warm-blooded animal subjected to barbituate anesthesia to potentiate effects thereof wherein there is administered to the warm-blooded animal a therapeutically effective amount of a composition selected from the group consisting of 5-methyl-3-sulfanilamidoisoxazole, a salt of 5-methyl-3-sulfanilamidoisoxazole with a pharmaceutically acceptable base, 2,4-diamino-5-3-(3,4,5-trimethoxybenzyl) pyrimidine, a salt of 2,4-diamino-5-(3,4,5-trimethoxybenzyl) pyrimidine with a pharmaceutically acceptable acid and mixtures thereof.Type: GrantFiled: September 27, 1984Date of Patent: April 28, 1987Assignee: University of Medicine and Dentistry of New JerseyInventors: Charles R. Spillert, Corinne Devereux, Eric J. Lazaro
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Patent number: 4636494Abstract: Choline or a natural or synthetic compound that dissociates to form choline is administered to a patient concomitantly with a drug in order to potentiate the effect of the drug by increasing acetylcholine levels in the brain or other tissues, and/or to suppress, or block the development of, unwanted side effects of the drug, by increasing acetylcholine levels in the brain or other tissues.Type: GrantFiled: March 17, 1982Date of Patent: January 13, 1987Assignee: Massachusetts Institute of TechnologyInventors: John H. Growdon, Richard J. Wurtman
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Patent number: 4634707Abstract: Novel 5-pyrimidinecarboxamides useful for regressing or inhibiting the growth of leukemia and tumors in mammals. The compounds have the formula: ##STR1## wherein: R is hydrogen, 2- or 3-halo, 4-fluoro, 2-methyl, 2- or 4-alkoxy, or 2- or 4-trifluoromethyl, and R.sub.1 is hydrogen; orR is 2-fluoro and R.sub.1 is 4-fluoro; orR is 2-methoxy and R.sub.1 is 5-methyl; andR.sub.2 and R.sub.3 are hydrogen atoms or carbohydrate residues; and,with the exception of the compound wherein R is 4-methoxy and R.sub.1 is hydrogen, the pharmacologically acceptable acid-addition salts thereof.Type: GrantFiled: February 8, 1985Date of Patent: January 6, 1987Assignees: Uniroyal Chemical Company, Uniroyal Ltd.Inventors: Arthur D. Brewer, John A. Minatelli
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Patent number: 4628056Abstract: There are disclosed novel oxopyrimidine derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or lower alkyl optionally substituted by lower alkoxy, and R.sub.3 and R.sub.4 may be the same or different and are each phenyl optionally substituted by lower alkyl or halogen, provided that when R.sub.1 and R.sub.2 are both hydrogen, R.sub.3 and R.sub.4 are each substituted phenyl. Pharmaceutical compositions containing these compounds and their use as anticonvulsant, antianxiety and muscle relaxant agents are described.Type: GrantFiled: September 5, 1984Date of Patent: December 9, 1986Assignee: Taro Pharmaceutical Industries Ltd.Inventors: Barrie Levitt, Morris Stolar
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Patent number: 4557934Abstract: Improved topical pharmaceutical compositions containing a pharmaceutically-active agent and the penetration enhancing agent 1-dodecylazacycloheptan-2-one are disclosed. This agent is used at selected levels in combination with certain C.sub.3 -C.sub.4 diols or a 1-substituted azacycloalkyl-2-one. This composition provides marked transepidermal and percutaneous delivery of the selected pharmaceutically-active agent. A method of treating certain pathologies and conditions responsive to the selected active, systemically or locally, is also disclosed.Type: GrantFiled: June 21, 1983Date of Patent: December 10, 1985Assignee: The Procter & Gamble CompanyInventor: Eugene R. Cooper
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Patent number: RE32393Abstract: According to the invention, the parenteral administration of water-insoluble pharmacologically active agents is enhanced wherein the agents are administered in the lipoid phase of a carrier emulsion comprising a microemulsion of a finely dispersed lipoid in an aqueous phase. The lipoid preferably has a mean particle size below 1 micron. This makes it possible to administer water-insoluble agents in high concentrations, and thus a lower dose, whereby a rapid onset of the pharmacological effect is accompanied by a markedly reduced incidence of injury to body tissues.Type: GrantFiled: August 14, 1984Date of Patent: April 7, 1987Assignee: KabiVitrum ABInventors: Karl A. J. Wretlind, Stellan Ljungberg, Ivan Hakansson, Bengt M. Ajaxon