Additional Hetero Ring Patents (Class 514/444)
-
Patent number: 5234946Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.Type: GrantFiled: August 30, 1991Date of Patent: August 10, 1993Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
-
Patent number: 5227400Abstract: A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: April 3, 1992Date of Patent: July 13, 1993Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Ronald J. Beidiger
-
Patent number: 5208222Abstract: Avermectin derivatives are disclosed wherein the 4"-hydroxy group is replaced by a substituted alkylthio or acylthio group or an iodo group. These avermectin derivatives can be further derivatized at the 5- and 23-positions as ketoximes or O-substituted ketoximes. The 4"-substituted avermectin derivatives are prepared from the 4"- and 4'-trifluoromethanesulfonyl avermectin derivatives with halo- or sulfur-containing nucleophiles. The 4"- and 4'-.alpha.- and .beta.-trifluoromethane sulfonates are prepared selectively and converted into 4"- or 4'-alkyl- or acylsulfides, or iodides using the appropriate sulfur-containing or iodine nucleophile. Substituted sulfoxy and sulfonyl substituents at the 4"- and 4'-positions are prepared from oxidation of the corresponding substituted sulfides. The new compounds are potent anti-parasitic agents; in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.Type: GrantFiled: March 28, 1991Date of Patent: May 4, 1993Assignee: Merck & Co., Inc.Inventors: Peter T. Meinke, Helmut Mrozik
-
Patent number: 5206231Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.Type: GrantFiled: September 10, 1991Date of Patent: April 27, 1993Assignee: Sterling Drug Inc.Inventor: Robert E. Johnson
-
Patent number: 5204345Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 is hydrogen atom, an optionally substituted aliphatic hydrocarbon residue or an optionally substituted acyl group, or a salt thereof.The compound (I) of the invention has, among others, angiogenesis inhibiting activity, cell-proliferation inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.Type: GrantFiled: March 6, 1990Date of Patent: April 20, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoji Kishimoto, Takeshi Fujita
-
Patent number: 5192777Abstract: Compounds of formula (I) ##STR1## and salts thereof, wherein R.sup.1 represents a methyl, ethyl or ispropyl group; R.sup.2 represents a C.sub.2-7 alkyl group interrupted by an oxygen or sulphur atom or an aryl, aryl C.sub.1-7 alkyl or heteroaryl C.sub.1-7 alkyl group; OR.sup.3 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms; and the group .dbd.NOR.sup.2 is in the E configuration.These compounds may be used for controlling insect, acarine, nematode or other pests.Type: GrantFiled: December 11, 1990Date of Patent: March 9, 1993Assignee: American Cyanamid CompanyInventors: Michael V. J. Ramsay, Edward P. Tiley, Derek R. Sutherland
-
Patent number: 5185364Abstract: The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S;R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;R.sub.3 is loweralkyl;R.sub.4 is selected from ##STR2## wherein Y is O or S, R.sub.6 is hydrogen, methoxy or halo and m is 0 or 1l R.sub.5 is hydrogen, loweralkyl, phenyl or substituted phenyl wherein the phenyl ring is substituted with one, two or three substituents independently selected from loweralkyl, halo, hydroxy, loweralkoxy, amino and thioalkoxy; andR.sub.8 is hydrogen or R.sub.3 and R.sub.8 taken together form a pyrrolidine ring; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 31, 1991Date of Patent: February 9, 1993Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, David L. Arendsen, Robert E. Zelle
-
Patent number: 5183827Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 18, 1991Date of Patent: February 2, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
-
Patent number: 5180735Abstract: The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.Type: GrantFiled: August 29, 1990Date of Patent: January 19, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoji Kishimoto, Shogo Marui, Takeshi Fujita
-
Patent number: 5171742Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent and which has a 23-acyl cycloalkyl, phenyl or substituted hydroxymethyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with a 23-acyl substituent and new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 15, 1991Date of Patent: December 15, 1992Assignee: Merck & Co., Inc.Inventor: Peter T. Meinke
-
Patent number: 5145868Abstract: Substituted alkanophenones of the general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is a 5-membered heteroaryl radical that contains 1N, O or S atom as hetero atom and is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterfied or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties can e used as antiallergic active ingredients in medicaments.Type: GrantFiled: November 15, 1991Date of Patent: September 8, 1992Assignee: Ciba-Geigy CorporationInventors: Andreas von Sprecher, Andreas Beck
-
Patent number: 5143936Abstract: A benzopyran compound of the general formula (I) ##STR1## wherein A represents --OR.sup.1 or --NH--COR.sup.2 (wherein R.sup.1 represents hydrogen, a lower alkyl, formyl, an alkanoyl, an aroyl or an aralkyl and R.sup.2 represents hydrogen, a lower alkyl, a lower alkoxy, amino, mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl); R.sup.3 represents hydrogen, a lower alkyl, a lower alkoxy, amino, a mono- or di-lower alkylamino, an amino-lower alkyl, a hydroxy-lower alkyl, a halo-lower alkyl, a lower alkoxy-lower alkyl, an acyloxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an aryl or a heteroaryl, or R.sup.2 and R.sup.3 combinedly together form an alkylene having 1 to 2 carbon atoms; R.sup.4 and R.sup.5 are the same or different, and respectively represent hydrogen or a lower alkyl, or combinedly together form an alkylene having 2 to 5 carbon atoms; R.Type: GrantFiled: March 21, 1991Date of Patent: September 1, 1992Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Tsutomu Yamanaka, Toshio Seki, Tohru Nakajima, Osamu Yaoka
-
Patent number: 5134128Abstract: New 5-hydroxy-2-furanone compounds having anti-inflammatory, immunosuppressive and anti-proliferative activity and are useful in treating psoriasis and modifying calcium homeostasis.Type: GrantFiled: May 13, 1991Date of Patent: July 28, 1992Assignee: Allergan, Inc.Inventors: Gary C. M. Lee, Michael E. Garst, John N. Bonfiglio, Elizabeth T. Syage
-
Certain benzodioxole, benzodioxane and benzodioxepin derivatives useful as 5-lipoxygenase inhibitors
Patent number: 5120758Abstract: The invention relates to the compounds of the formula ##STR1## wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyloxy, or C.sub.3 -C.sub.7 -cycloalkyloxy; n represents 1, 2, 3 or 4; m represents 0, 1 or 2; A represents a direct bond or lower alkylene; X represents oxygen or sulfur; R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.Type: GrantFiled: July 8, 1991Date of Patent: June 9, 1992Assignee: Ciba-Geigy CorporationInventor: Yoshitaka Satoh -
Patent number: 5116848Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.Type: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
-
Patent number: 5114963Abstract: The present invention is a method for lowering serum levels of Lp(a), thereby reducing the risk of atherosclerotic disease. Specifically, the present invention comprises administering an effective amount of a N,S-diacyl-L-cysteine to a human or animal with elevated serum levels of Lp(a). The N,S-diacyl-L-cysteines comprise a compound selected from the group having the formula: ##STR1## wherein R is selected from the group consisting of hydrogen and an alkyl group containing 1 to 8 carbon atoms and R' is selected from the group consisting of acetyl, benzoly, thenoyl, 2-chromone-carbonyl and succinyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 13, 1991Date of Patent: May 19, 1992Assignee: Medicis CorporationInventors: John W. Holaday, Jonah Shacknai, Leonard L. Mazur
-
Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
-
Patent number: 5112853Abstract: New furanone compounds have anti-inflammatory, immunosuppresive and anti-proliferative activity and are useful in treating psoriasis and modifying calcium homeostasis. A compound of the invention is 4-[3,6-dihydro-6-hydroxy-5-(3-phenylpropyl)-2H-pyran-2-yl]-5-hydroxy-2-(5H )-furanone.Type: GrantFiled: June 3, 1991Date of Patent: May 12, 1992Assignee: Allergan, Inc.Inventors: Michael E. Garst, Elizabeth T. Syage
-
Patent number: 5110821Abstract: Compounds of the formula ##STR1## wherein: Y is an alkylene bridge of 3-9 carbon atoms;R' is lower-alkyl or hydroxy-lower-alkyl or 1-5 carbon atoms;R.sub.1 and R.sub.2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; andR.sub.8 is hydrogen or lower-alkyl of 1-5 carbon atoms, with the proviso that when R.sub.8 is hydrogen R' is hydroxy-lower-alkyl,are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.Type: GrantFiled: June 7, 1990Date of Patent: May 5, 1992Assignee: Sterling Drug Inc.Inventor: Guy D. Diana
-
Patent number: 5110831Abstract: The present invention relates to vinylogous hydroxamic acids, processes for their manufacture, pharmaceutical preparations containing them, and their use in the treatment of various disorders.Type: GrantFiled: November 30, 1990Date of Patent: May 5, 1992Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Ronald L. Magolda, Stephen W. Wright
-
Patent number: 5104869Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.Type: GrantFiled: October 25, 1990Date of Patent: April 14, 1992Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Charles Frederick, Jeremy I. Levin, Fuk-Wah Sum, Marvin F. Reich
-
Patent number: 5104871Abstract: Compounds of formula (I) ##STR1## and salts thereof, wherein R is a C.sub.1-4 alkyl group, R.sup.1 is a methyl, ethyl or isopropyl group; and OR.sup.2 is a hydroxyl or substituted hydroxyl group having up to 25 carbon atoms.These compounds may be used for controlling insect, acarine, nematode or other pests.Type: GrantFiled: September 9, 1988Date of Patent: April 14, 1992Assignee: American Cyanamid CompanyInventors: Richard Bell, Michael V. J. Ramsay, Hazel M. Noble, David Noble, Neil Porter, John B. Ward, Richard A. Fletton
-
Patent number: 5100911Abstract: Thienyloxyalkylamine derivatives of the general formula: ##STR1## wherein --O--CH.sub.2 --CH.sub.2 --NR.sub.2 R.sub.3 is in position 4 or 5 of the thiophene ring;R.sub.1 is hydrogen, halogen, CF.sub.3, alkyl or alkoxy;R.sub.2 and R.sub.3 are the same or different and are each alkyl, cycloalkyl, alkenyl or alkynyl each having up to 8 C atoms, or NR.sub.2 R.sub.3 is a 5 to 7-membered saturated heterocyclic ring optionally containing a further hetero atom which is oxygen or nitrogen optionally substituted by an alkyl group having 1 to 3 C atoms; andn is an integer of 1 to 5; as well as their acid addition salts, are suitable for treatment of heart rhythm disturbances.Type: GrantFiled: May 15, 1990Date of Patent: March 31, 1992Assignee: Ebewe Arzneimittel Gesellschaft m.b.H.Inventors: Dieter Binder, Gerhard Greier, Franz Rovenszky, Friedrich Hillebrand
-
Patent number: 5096905Abstract: The invention relates to elaiophylin derivatives of the formulae (I), (I'), (III) and (III') ##STR1## in which the C.dbd.C double bonds in the 2,3 and 4,5 position may also be hydrogenated and in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings indicated. The invention furthermore relates to a process for the preparation of these elaiophylin derivatives, and the use thereof as pharmaceuticals, in particular as anthelmintic pharmaceuticals.Type: GrantFiled: September 14, 1989Date of Patent: March 17, 1992Assignee: Hoechst AktiengesellschaftInventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein
-
Patent number: 5089509Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-2; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 20, 1989Date of Patent: February 18, 1992Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
-
Patent number: 5084464Abstract: The present invention provides conjugated .gamma.-hydroxybutenolide compounds represented by the general formula: ##STR1## wherein R represents, when n is 1, furyl groups, thienyl groups or naphthyl groups, unsubstituted or substituted with alkyl group or alkoxy group; phenyl groups substituted with dialkylamino group, acyl group or pyridinyl group; or ##STR2## when n is 2 or 3, phenyl groups unsubstituted or substituted with alkyl group or alkoxy group; and antiulcer agents comprising an aforementioned conjugated .gamma.-hydroxybutenolide compound as an active ingredient.Type: GrantFiled: September 13, 1990Date of Patent: January 28, 1992Assignee: Kuraray Company Ltd.Inventors: Yoshin Tamai, Masahiro Torihara, Yoichi Kido, Johji Yamahara
-
Patent number: 5077303Abstract: Esters of the general formula I ##STR1## where A is hydrogen, alkyl, cycloalkyl, cycloalkenyl, naphthyl, biphenyl, hetaryl or phenyl, these radicals being substituted or unsubstituted, and X is CH or N, and fungicides containing these esters.Type: GrantFiled: March 22, 1990Date of Patent: December 31, 1991Assignee: BASF AktiengesellschaftInventors: Rainer Seele, Franz Schuetz, Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
-
Patent number: 5071871Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.Type: GrantFiled: July 10, 1990Date of Patent: December 10, 1991Assignee: Sandoz Ltd.Inventors: Stefan Blarer, John Morley, Ian D. Chapman
-
Patent number: 5068237Abstract: Substituted furans and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive, dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: May 21, 1990Date of Patent: November 26, 1991Assignee: Warner-Lambert CompanyInventor: Sheila H. Hobbs
-
Patent number: 5064827Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.Type: GrantFiled: August 23, 1990Date of Patent: November 12, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
-
Patent number: 5064830Abstract: Certain derivatives of oxophthalazinyl acetic acids of the formula ##STR1## wherein R.sub.1 is hydroxy or a prodrug group, and R.sub.2 and R.sub.3 are independently hydrogen, fluoro, chloro or trifluoromethyl, except that R.sub.2 and R.sub.3 are not both hydrogen, or a pharmaceutically acceptable base addition salt of a compound of formula I wherein R.sub.1 is hydroxy, are capable of lowering blood uric acid levels in mammals. These oxophthalazinyl acetic acid derivatives are for instance useful for treating gout and gouty arthritis in a mammal .Type: GrantFiled: August 2, 1990Date of Patent: November 12, 1991Assignee: Pfizer Inc.Inventor: Paden C. Going
-
Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
-
Patent number: 5053430Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.Type: GrantFiled: September 22, 1989Date of Patent: October 1, 1991Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
-
Patent number: 5045563Abstract: A method is provided herein for controlling insects which are harmful to agriculture and forestry and which are also harmful both to humans and to domestic animals. The method involves the steps of applying to a locus infested with such insects, a composition comprising a carrier and a biocidal-amount of a specifically-recited phototoxic, naturally-occurring thiophene, acetylene, or a synthetic, structurally-related derivative, analogue or acetylenic compound. Then, that composition, while at that locus, is subjected to UV radiation in the range of about 300 nm to about 400 nm, for a sufficient time to impart, to such phototoxic naturally-occurring thiophene, acetylene, or synthetic structurally-related derivative, analogue or acetylenic compound the desired insect control activity. Certain of these phototoxic naturally-occurring thiophenes, or acetylenes or synthetic, structurally-related compounds are also novel and provide novel insect control compositions.Type: GrantFiled: August 26, 1986Date of Patent: September 3, 1991Assignee: Her Majesty the Queen in right of Canada, as represented by Minister of National Defence of Her Majesty's Canadian GovernmentInventors: Peter Morand, John T. Arnason, Bernard J. R. Philogene, Anita M. MacEachern, Leonard C. Leitch, Jerzy Kaminski
-
Patent number: 5041444Abstract: A benzoxepin derivative represented by the formula (I): ##STR1## wherein R represents a heterocyclyc group, and salts thereof; a process for production thereof comprising the steps of reducing an oxime represented by the formula (V): ##STR2## wherein R has the same meaning as defined in the formula (I), and hydrolyzing the intermediate produced of the above reduction; and pharmaceuticals comprising the compound (I).Type: GrantFiled: March 8, 1990Date of Patent: August 20, 1991Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Makoto Shibata
-
Patent number: 5041461Abstract: A pharmaceutically-active compound of the formula ##STR1## in which R.sup.1 is C.sub.1-4 alkythio, C.sub.1-4 alkylsulphinyl or C.sub.1-4 alkylsulphonyl, R.sup.2 is C.sub.1-4 alkyl, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.Type: GrantFiled: September 26, 1989Date of Patent: August 20, 1991Assignee: Lilly Industries LimitedInventors: Maria I. Fernandez Fernandez, Terrence M. Hotten, David E. Tupper
-
Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
-
Patent number: 5036098Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.Type: GrantFiled: September 14, 1989Date of Patent: July 30, 1991Assignee: Nippon Shinyaku Co., Ltd.Inventors: Kiyoshi Kimura, Masahiro Kise, Iwao Morita
-
Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
-
Patent number: 5025017Abstract: Seco-mevinic acid derivatives are provided which has the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis. New intermediates for preparing the above seco-mevinic acid derivatives are also provided.Type: GrantFiled: September 28, 1989Date of Patent: June 18, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Donald S. Karanewsky
-
Patent number: 5021458Abstract: Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as above; Y is selected from the group consisting of ##STR4## R.sup.1 is hydrogen atom or an alkyl group; R.sup.2 is hydrogen atom or an alkyl group; R.sup.3 is hydrogen atom, a halogen atom or an alkyl group; R.sup.4 is hydrogen atom, an alkyl group, a cycloalkyl group, a halogenated alkyl group or a halogen atom; R.sup.5 is hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, nitro group or hydroxy group; R.sup.5 is attached to an arbitrary position of X, and R.sup.3 or R.sup.4 is attached to an arbitrary position of Y.The amine derivatives (I) are useful as fungicides.Type: GrantFiled: December 7, 1988Date of Patent: June 4, 1991Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Tetsuya Maeda, Toshiyuki Yamamoto, Mituo Takase, Kazuya Sasaki, Tadashi Arika, Mamoru Yokoo, Rieko Hashimoto, Kouji Amemiya, Sakae Koshikawa
-
Patent number: 5021449Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1 is --CHO, CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.2 is C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl or --COOH, R.sup.3 is C.sub.1-4 alkyl and X is pyrrolidinyl or pyrrolidinylmethyl; and salts and esters thereof.Type: GrantFiled: September 26, 1989Date of Patent: June 4, 1991Assignees: Lilly S.A., Lilly Industries LimitedInventors: Maria I. Fernandez Fernandez, Terrence M. Hotten, David E. Tupper
-
Patent number: 5017601Abstract: A compound of the formula: ##STR1## in which R is alkyl, phenyl or halophenyl; R.sup.2 is substituted phenyl having from 1 to 3 substituents selected from halo, alkyl, alkythio, alkylsulfonyl, cyano, trifluoromethyl, or R.sup.2 is pyridinyl, pyrazinyl, quinolinyl, N-alkylpyrrolyl, thienyl, benzothienyl, or furyl; and n is 1 or 2, are cytoprotective anti-ulcer agents.Type: GrantFiled: August 23, 1990Date of Patent: May 21, 1991Assignee: American Home Products CorporationInventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
-
Patent number: 5015656Abstract: A pharmaceutical compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, hydroxy, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, --CHO, --CH.sub.2 OH, --CH.sub.2 OC.sub.1-4 alkyl, --COOH, --COC.sub.1-3 alkyl, --CH(OH)C.sub.1-3 alkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkenyloxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphinyl, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge; provided that at least one of R.sup.2 and R.sup.3 is C.sub.1-4 alkoxy or C.sub.2-4 alkenyloxy; and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.Type: GrantFiled: September 26, 1989Date of Patent: May 14, 1991Assignees: Lilly S.A., Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
-
Patent number: 5015661Abstract: Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.Type: GrantFiled: June 16, 1989Date of Patent: May 14, 1991Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
-
Novel 7-aroyl-4-hydroxy-3-methyl-benzofurans as dual inhibitors of cyclooxygenase and 5-lipoxygenase
Patent number: 5006549Abstract: Novel 7-Aroyl-4-Hydroxy-3-Methyl-Benzofurans of the following general formula (I) are disclosed: ##STR1##The compounds are found to be potent dual inhibitors of cyclooxygenase and 5-lipoxygenase.Type: GrantFiled: May 24, 1989Date of Patent: April 9, 1991Assignee: Merck & Co., Inc.Inventors: Robert A. Zambias, Milton L. Hammond -
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
-
Patent number: 5001145Abstract: Compounds are described of formula (1) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 represents a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom or a C.sub.1-8 alkyl group and the group >C.dbd.NOR.sup.5 is in the E configuration).These compounds may be used for controlling insect, acarine, nematode or other pests.Type: GrantFiled: January 27, 1989Date of Patent: March 19, 1991Assignee: American Cyanamid CompanyInventors: Michael V. J. Ramsay, Derek N. Evans, Derek R. Sutherland, Edward P. Tiley, John B. Ward, Neil Porter, Hazel M. Noble, Richard A. Fletton, David Noble
-
Patent number: 4997820Abstract: Novel macrocyclic compounds of the formual I ##STR1## where the dotted line in the 9,10-position is a saturated bond or a double bond, alternatively, and R is hydrogen, methyl or certain acyl radicals, and R.sub.o is hydrogen, halogen, azido, thiol, hydroxyl or --OY, where Y is, among other radicals, an ether radical, a silyl group, a sulfonyl group, a sugar radical or a (thiol)acyl radical, and R being methyl if there is a double bond in the 9,10-position, have microbicidal properties for the control of phytopathogenic microorganisms. They can be employed in the customary formulation for the control of plant disease.Type: GrantFiled: September 8, 1989Date of Patent: March 5, 1991Assignees: Gesellschaft fur Biotechnologische Forschung mbH, Ciba-Geigy CorporationInventors: Marius Sutter, Norbert Bedorf, Gerhard Hofle, Dietmar Schummer, Bettina Bohlendorf
-
Patent number: 4996227Abstract: Heterocyclic diones of the class containing 3-(heteroarylalkylene)- and 3(arylalkylene)-2, 4 (3H, 5H)-furandiones, and 3-(heteroarylalkylene)-pyrrolidene diones and -thiophene diones are disclosed as being effective cancer chemotherapy drugs, some of which are themselves novel compounds. Various members of this class were tested both in vitro and in vivo to demonstrate their effectiveness at reducing or inhibiting cancer tumor cells. The class of drugs was evaluated against a series of 10 human tumors in the in vitro Human Tumor Cell Assay procedure. The procedure indicates that this class of heterocyclic diones is effective against a broad variety of types of cancer and has little or no toxic effects based upon hematological and pathological evaluations.Type: GrantFiled: February 24, 1989Date of Patent: February 26, 1991Assignee: University of CincinnatiInventors: Hans W. Zimmer, Orlando J. Martelo, Robert S. Franco