Benzene Ring Containing Patents (Class 514/637)
-
Patent number: 5710166Abstract: Novel N-Acyl Beta Amino Acid derivatives of the formula ##STR1## are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.Type: GrantFiled: August 24, 1995Date of Patent: January 20, 1998Assignee: The Monsanto CompanyInventors: Foe S. Tjoeng, Mihaly V. Toth
-
Patent number: 5686496Abstract: The new compound of formula ##STR1## may be prepared by conventional methods and used therapeutically as an LTB.sub.4 -receptor antagonist.Type: GrantFiled: March 28, 1997Date of Patent: November 11, 1997Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Armin Fugner, Hubert Heuer, Christopher Meade
-
Patent number: 5637621Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: June 10, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
-
Patent number: 5632999Abstract: The invention comprises a method of controlling fleas which includes continuously administering to the haircoat of a homeothermic animal an ovicidally effective amount of 2-(1-methyl-2-(4-phenoxyphenoxy)ethoxy)pyridine (pyriproxifen) from a sustained release matrix at a rate of 0.1 mcg/kg/day to 100 mcg/kg/day. The method may also include the use of additional ingredients such as insecticides, plasticizers, lubricants and antioxidants in a sustained release matrix.Type: GrantFiled: August 18, 1993Date of Patent: May 27, 1997Assignee: Virbac, Inc.Inventor: Thomas A. Miller
-
Patent number: 5629348Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.Type: GrantFiled: November 14, 1994Date of Patent: May 13, 1997Assignee: NZYM, Inc.Inventors: Joel Bolonick, Terrance J. Leighton, Ida K. Yu
-
Patent number: 5552443Abstract: N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.Type: GrantFiled: January 18, 1994Date of Patent: September 3, 1996Assignees: Oregon Health Sciences University, The University of OregonInventors: John F. W. Keana, Eckard Weber
-
Patent number: 5527823Abstract: A formulation suitable for spraying or for dilution with water to form a sprayable preparation, the formulation comprising an active ingredient, optionally a carrier or solvent for the active ingredient, an emulsifier and an evaporation retardant, characterized in that the formulation satisfies formula ##EQU1## where L is less than or equal to 15, A=700376, B=-1.51, C=0.8472, M.sub.oil is the weighted average relative molar mass of the oil phase M.sub.retardant is the weighted average relative molar mass of the retardant, and X=(M.sub.oil) 1.8/Y, where Y is the molar solubility ration of the formulation, defined as the minimum number of moles of the oil phase which will dissolve the retardant, divided by the number of moles of retardant, provided that, in the formula above, any solvent which has no liquid phase at 27.degree. C. at atmospheric pressure is excluded. The formulation may comprise a pesticide or herbicide. The action of the evaporation retardant is improved.Type: GrantFiled: February 8, 1994Date of Patent: June 18, 1996Assignee: Roussel UCLAFInventors: Robert Martin, David A. Jeffries, Denise K. North, John M. Groome, Peter L. Crampton, Andrew J. Huson
-
Patent number: 5462969Abstract: The present invention provides methods for treating and preventing the onset of Pneumocytis carinii pneumonia (PCP) comprising administering to a mammal in need of such treatment or prevention an effective amount of a pharmaceutically acceptable iron chelator. This invention also provides a method for treating or preventing the onset of PCP comprising administering to a mammal in need of such treatment or prevention a composition comprising the following components: (a) a pharmaceutically acceptable iron chelator; (b) a compound selected from trimethoprim/sulfamethoxazole and pentamidine; and (c) a pharmaceutically compatible carrier or diluent, wherein the amounts of said component (a) and said component (b) in combination are effective in treating said pneumonia. Also provided is a composition for the treatment or prevention of PCP.Type: GrantFiled: February 4, 1994Date of Patent: October 31, 1995Assignee: New York UniversityInventors: Allen B. Clarkson, Jr., Robert W. Grady
-
Patent number: 5366726Abstract: A method of preventing clinically manifest Pneumocystis carinii pneumonia in immunocompromised humans is provided wherein an aerosol of pentamidine is administered to the patient in a manner which delivers the aerosol to the patient's alveoli. Also provided is a method of treating Pneumocystis carinii pneumonia in HIV seropositive individuals comprising administering a therapeutically effective amount of pentamidine aerosol to the HIV positive individual through inhalation. In addition, a method is provided of administering pentamidine to a human comprising aerosolizing a pentamidine solution in a nebulizer system having a one-way valve disposed between the nebulizer and the mouthpiece of the nebulizer system.Type: GrantFiled: July 23, 1992Date of Patent: November 22, 1994Assignee: The Regents of the University of CaliforniaInventors: Robert J. Debs, Alan B. Montgomery, John E. Conte, Jeffrey A. Golden
-
Patent number: 5364868Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.Type: GrantFiled: February 11, 1993Date of Patent: November 15, 1994Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Hans-Jochen Lang, Wolfgang Scholz, Wolfgang Linz, Udo Albus
-
Patent number: 5364615Abstract: A method of preventing clinically manifest Pneumocystis carinii pneumonia in immunocompromised humans is provided wherein an aerosol of pentamidine is administered to the patient in a manner which delivers the aerosol to the patient's alveoli. Also provided is a method of treating Pneumocystis carinii pneumonia in HIV seropositive individuals comprising administering a therapeutically effective amount of pentamidine aerosol to the HIV positive individual through inhalation. In addition, a method is provided of administering pentamidine to a human comprising aerosolizing a pentamidine solution in a nebulizer system having a one-way valve disposed between the nebulizer and the mouthpiece of the nebulizer system.Type: GrantFiled: August 13, 1992Date of Patent: November 15, 1994Assignee: Regents of the University of CaliforniaInventors: Robert J. Debs, Alan B. Montgomery, John E. Conte, Jeffrey A. Golden
-
Patent number: 5360810Abstract: There is disclosed a compound of the formula (I): ##STR1## wherein X is a hydrogen atom or 1 to 5 substituents which may be the same or different and are selected from the group consisting of a hydrogen atom, alkyl, alkenyl, alkynyl, optionally substituted phenyl, an optionally substituted heterocyclic group, alkoxy, alkenyloxy, alkynyloxy, optionally substituted phenoxy, mono-, di- or tri-substituted halogenoalkyl and a halogen atom; Y is CH or N; m is 0 or 1; A is a group of the formula: ##STR2## (wherein R.sup.1 is a hydrogen atom or alkyl; n is 0 or 1; B is O, S or NR.sup.3 ; R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, alkyl, alkenyl, alkynyl, phenyl, benzyl, acyl or phenacyl). There are also disclosed the production thereof and an agricultural fungicide containing the compound as an active component.Type: GrantFiled: March 18, 1993Date of Patent: November 1, 1994Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Hideyuki Takenaka, Norihiko Tanimoto, Michio Masuko, Toshihiko Takahashi
-
Patent number: 5344841Type: GrantFiled: June 8, 1992Date of Patent: September 6, 1994Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
-
Patent number: 5308869Abstract: N,N'-disubstituted-amidines, e.g., of the formula ##STR1## wherein R, R' and R" are substituted or unsubstituted hydrocarbon and/or heterocyclic groups.Methods are provided for the treatment or prophylaxis of anxiety in an animal, for treating psychosis, and for treating hypertension by administering an effective amount of an N,N'-disubstituted amidine which, preferably, has a high affinity for the sigma receptor.Type: GrantFiled: March 30, 1992Date of Patent: May 3, 1994Assignee: State of Oregon, acting by and through the Oregon State Board of Higher EducationInventors: John F. W. Keana, Eckard Weber
-
Patent number: 5286752Abstract: Novel diarylamidines, and compositions and methods for treating cardiac arrhythmias in mammals utilizing the novel and related known diarylamidines of formula I, II, III and IV ##STR1##Type: GrantFiled: September 10, 1991Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Robert E. Johnson, Thomas E. D'Ambra
-
Patent number: 5246965Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which:R is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;R.sub.1 is a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical and a cycloaliphatic hydrocarbon radical;X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); andX.sub.Type: GrantFiled: September 17, 1992Date of Patent: September 21, 1993Assignee: Ciba-GeigyInventor: Alan J. Main
-
Patent number: 5230897Abstract: Pharmaceutical compositions and transdermal patches comprised of pentamidine and a penetration enhancing amount of a terpene selected from the group consisting of menthol, carvone, carveol, dihydrocarveol, dihydrocarvone, neomenthol, isopulegol, terpene-4-ol, menthone, pulegol, camphor, geraniol, .alpha.-terpineol, citral, linalol, carvacrol, thymol and anethole are disclosed for delivery of a therapeutically effective amount of pentamidine or its pharmaceutically acceptable salts.Type: GrantFiled: October 31, 1991Date of Patent: July 27, 1993Assignee: G. D. Searle & Co.Inventors: Martin J. Griffin, Tugrul T. Kararli, Stanley C. Penzotti, Jr., Rachelle M. Rydzik, Cynthia M. Schmidt
-
Patent number: 5204370Abstract: The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.Type: GrantFiled: November 5, 1990Date of Patent: April 20, 1993Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
-
Patent number: 5183828Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.Type: GrantFiled: July 20, 1990Date of Patent: February 2, 1993Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
-
Patent number: 5026687Abstract: A preferred method and dosages for the short and long-term treatment of human retroviral infections, or retroviral-like infections, including acquired immunodeficiency syndrome (AIDS) and other manifestations of human immunodeficiency virus (HIV) infection, with 2',3'-dideoxyinosine (ddl) are disclosed, along with a protocol for halting and restarting 2',3'-dideoxyinosine to minimize certain side effects.Type: GrantFiled: January 3, 1990Date of Patent: June 25, 1991Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Robert Yarchoan, Hiroaki Mitsuya, Samuel Broder
-
Patent number: 4938797Abstract: The invention relates to a process for the preparation of microcapsules having a capsule wall of polyurea and encapsulating a water-immiscible pesticide. The process comprises first dispersing a solution of a polyisocyanate in the sparingly water-soluble pesticide, in the presence of an anionic dispersant and at least one nonionic protective colloid and/or a nonionic surfactant, and subsequently reacting the dispersion with a polyamine, to give a stable aqueous suspension of microcapsules which can be used either direct or after dilution with water as pesticidal composition.Type: GrantFiled: June 7, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Hans W. Hasslin, Michael J. Hopkinson
-
Patent number: 4775695Abstract: This invention relates to novel substituted amidinoalkoxy and amidinoalkylamino indanones and salts thereof. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, the neurological problems caused by AIDS, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions, and elevated intracranial pressure.Type: GrantFiled: June 1, 1987Date of Patent: October 4, 1988Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
-
Patent number: 4710512Abstract: Liquid formulations of the pesticide amitraz are stabilized by the addition of one or more aluminum alkoxides.Type: GrantFiled: October 14, 1986Date of Patent: December 1, 1987Assignee: Schering Agrochemicals LimitedInventor: Michael A. Webb
-
Patent number: 4690947Abstract: Arthropodicidal compositions in the form of synergistic combinations of (A) cyano-(4-fluoro-3-phenoxyphenyl)-methyl 3-(2,2-dichlorovinyl)-2,2-dimethyl-cyclopropanecarboxylate plus (B) O-ethyl-O-[4-(methylthio)-phenyl]-S-propyl phosphorodithioate, (A) plus (C) N.sup.1 -(4-chloro-O-tolyl)-N,N-dimethylformamidine, (A) plus (B) plus (C), (A) plus (D) 1-(tricyclohexylstannyl)-1H-1,2,4-triazole, (A) plus (E) tricyclohexyl hydroxystannane, or (A) plus (F) hexakis-(2-methyl-2-phenylpropyl)-distannoxane, which are individually known compounds, which combinations possess synergistic arthropidicidal properties especially for the control of mites.Type: GrantFiled: November 25, 1985Date of Patent: September 1, 1987Assignee: Mobay CorporationInventors: Walter M. Zeck, Donald E. Simonet
-
Patent number: 4678775Abstract: A method of controlling a pest which comprises bringing into contact with the pest a pest-controlling amount of an agent selected from the group consisting of(1) a non-formamidine -p-octopamine agonist having substantial activity toward an octopamine receptor present in the pest;(2) a compound directly and substantially stimulating the enzyme, adenylate cyclase; and(3) a cyclic adenosine monophosphate (cAMP) analogue.Type: GrantFiled: May 1, 1984Date of Patent: July 7, 1987Inventor: James A. Nathanson
-
Patent number: 4661522Abstract: The present invention is dealing with cycloalkane-indene-carboximidamide derivatives having the general formula: ##STR1## wherein Rx together with either Ry.sub.1 or Ry.sub.2 represent the moiety ##STR2## (the other Ry being hydrogen), n represents the number 1, 2 or 3,R represents hydrogen or a (1-4 C)-alkyl group,R.sub.1 represents hydrogen, (1-4 C)-alkyl, hydroxyl, (1-4 C)-alkoxy or an amino group which is unsubstituted or substituted by (1-4 C)-alkyl andR.sub.2 is hydrogen, hydroxyl or (1-4 C)-alkyl,as well as the pharmaceutically acceptable salts thereof, with powerful blood platelet aggregation-inhibiting activity.Type: GrantFiled: May 15, 1985Date of Patent: April 28, 1987Assignee: Akzo N.V.Inventor: Tom Beetz
-
Patent number: 4634705Abstract: Disclosed herein are adrenergic compounds represented by the formula ##STR1## wherein m is 0, 1 or 2; R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are taken from the group consisting of hydrogen, hydroxy, loweralkyl, loweralkoxy, halo, amino, acetamido or NHSO.sub.2 R wherein R is taken from the group consisting of hydrogen or loweralkyl, provided that R.sub.1, R.sub.2, R.sub.3 and R.sub.7 cannot simultaneously be hydrogen or halo, and provided that when one of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 is halo, the others cannot simultaneously be hydrogen and when two of R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are halo, the other two cannot simultaneously be hydrogen and provided that R.sub.1 and R.sub.7 cannot simultaneously be methoxy each when R.sub.2 and R.sub.3 are hydrogen; R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.7 taken together can form a methylenedioxy or ethylenedioxy bridge; or R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 or R.sub.3 and R.sub.Type: GrantFiled: March 7, 1986Date of Patent: January 6, 1987Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Fatima Z. Basha
-
Patent number: 4623659Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.Type: GrantFiled: May 23, 1983Date of Patent: November 18, 1986Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
-
Patent number: 4598077Abstract: Amidine derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or a lower alkyl group, or R.sub.1 and R.sub.2 together with an intermediary carbon atom and/or hetero atom may form a ring; X represents ##STR2## (wherein R.sub.8 represents a hydrogen atom, a lower alkyl group, or --CH.sub.2 COOR.sub.9, where R.sub.9 represents a hydrogen atom or a lower alkyl group; Z represents a single bond, --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--); R.sub.3 represents a hydrogen or chlorine atom, methoxy group, nitro group, or amino group; Y represents --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 O--, or --OCH.sub.2 --; R.sub.4 represents a hydrogen atom, methoxy group, benzoyl group, nitro group, or amino group; and R.sub.5, R.sub.6 and R.sub.Type: GrantFiled: December 14, 1984Date of Patent: July 1, 1986Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Takuo Sato, Hiroyuki Kawamura, Takashi Yaegashi, Masateru Kurumi, Takuo Aoyama
-
Patent number: 4596811Abstract: The invention relates to special heterocyclic compounds corresponding to general tautomeric formula I which are distinguished by improved antagonistic activity on histamine-H.sub.2 -receptors. The invention also relates to a process for producing these compounds and to medicaments containing them.Type: GrantFiled: October 18, 1983Date of Patent: June 24, 1986Assignee: Ludwig Heumann & Co., GmbHInventors: Istvan Szelenyi, Stefan Postius, Helmut Schickaneder, Herbert Hansen
-
Patent number: 4543352Abstract: A class of naphthalene aminoalkylene ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.Type: GrantFiled: April 29, 1983Date of Patent: September 24, 1985Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
-
Patent number: 4539319Abstract: Compounds of formula (I) ##STR1## and acid addition salts thereof, whereinR.sup.1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy;andone of R.sup.2, R.sup.3 and R.sup.4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl;orR.sup.2 is hydrogen and ##STR2## is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.Type: GrantFiled: June 14, 1983Date of Patent: September 3, 1985Assignee: Beecham Group p.l.c.Inventors: Peter M. Newsome, Noel A. Mullan, John P. Marshall