Ortho Fused Patents (Class 560/28)
-
Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
-
Patent number: 5470977Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: March 14, 1995Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
-
Patent number: 5461147Abstract: Disclosed are a process and intermediates of the formula ##STR1## wherein R is --CH.sub.3 or --C(O)--OR.sup.1, and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5 ; or the formula ##STR2## wherein: R.sup.2 is H or OH, R is --C(O)OR.sup.1 and R.sup.1 is C.sub.1 -C.sub.6 alkyl or --CH.sub.2 C.sub.6 H.sub.5, or where R.sup.2 is H, R can also be CH.sub.3 ; for preparing benzazepine intermediates of the formula ##STR3## The benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.Type: GrantFiled: September 27, 1993Date of Patent: October 24, 1995Assignee: Schering CorporationInventors: Donald Hou, Richard W. Draper, Gary M. Lee, Janet L. Mas
-
Patent number: 5459149Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.Type: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
-
Patent number: 5457108Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.Type: GrantFiled: September 17, 1993Date of Patent: October 10, 1995Assignee: Bayer AktiengesellschaftInventors: Hanno Wild, Jutta Hansen, Jorg Lautz, Arnold Paessens
-
Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes
Patent number: 5426229Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: December 16, 1993Date of Patent: June 20, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus -
Patent number: 5399588Abstract: The compounds of this invention which have the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;X is --CH.sub.2 -- or --OCH.sub.2 --;n is 1 or 2;or a pharmaceutically acceptable salt thereof,are useful in treating or inhibiting the long-term complications of diabetes such as diabetic retinopathy, nephropathy and neuropathy through the inhibition of the enzyme aldose reductase. Aldose reductase inhibitors have been shown to prevent the biochemical, functional and morphological changes induced by hyperglycemia.Type: GrantFiled: December 14, 1993Date of Patent: March 21, 1995Assignee: American Home Products CorporationInventor: Michael S. Malamas
-
Patent number: 5371267Abstract: Amino acid derivatives of the general formula (I) ##STR1## are disclosed. The active compounds are suitable for use as plant protection agents, in particular as fungicides.Type: GrantFiled: October 16, 1992Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Wolfgang Bender, Heinz-Wilhelm Dehne
-
Patent number: 5359120Abstract: The invention provides compounds of the formula XX: M-Ar-CONH-R, where Ar represents an aromatic ring system, R-NH is the residue of an .alpha.-amino acid R-NH.sub.2 or oligopeptide R-NH.sub.2 and contains at least one carboxylic acid group in the form of a tertiary butyl ester and M represents a nitrogen mustard group of formula (a), where Y and L, which may be the same or different in a molecule, are leaving groups. The compounds are useful intermediates for the production of nitrogen mustard prodrugs.Type: GrantFiled: May 6, 1991Date of Patent: October 25, 1994Assignee: Cancer Research Campaign Technology LimitedInventor: Caroline J. Springer
-
Patent number: 5331006Abstract: Novel unnatural dipeptoids useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as antipsychotics are disclosed. Further, the compounds are antianxiety agents and antiulcer agents. The compounds are agents useful for preventing the response to withdrawal from chronic treatment or use of nicotine, diazepam, alcohol, cocaine, caffeine, and opioids. The compounds are also useful in treating and/or preventing panic attacks. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare diagnostic compositions.Type: GrantFiled: July 12, 1991Date of Patent: July 19, 1994Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Julian Aranda, Corinne Augelli-Szafran, Hans-Jurgen Betche, Ann Holmes, Michael D. Mullican, Martyn C. Pritchard, Reginald S. Richardson, Edward Roberts, Bruce D. Roth, Bradley D. Tait, Bharat K. Trivedi, Uwe Trostmann, Paul C. Unangst
-
Patent number: 5312831Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 12, 1993Date of Patent: May 17, 1994Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
-
Patent number: 5306842Abstract: A method for manufacturing a purified aromatic urethane. Aromatic urethanes are synthesized from a N,N'-disubstituted urea and an organic hydroxyl compound in a reaction medium. The organic hydroxyl compound and the primary aromatic amine side product which are present in the reaction mixture is distilled off and removed from the reaction mixture leaving a distillation bottom. The N,N'-disubstituted urea is separated and removed from the distillation bottom by solvent extraction of the aromatic urethane, and the aromatic urethane in the extract phase obtained in said solvent extraction is separated and purified.Type: GrantFiled: April 29, 1992Date of Patent: April 26, 1994Assignee: NKK CorporationInventors: Takao Ikariya, Masanori Itagaki, Masatsugu Mizuguchi, Makoto Miyazawa, Sachiko Yamamoto
-
Patent number: 5286753Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: April 16, 1993Date of Patent: February 15, 1994Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus
-
Patent number: 5272144Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.Type: GrantFiled: June 13, 1991Date of Patent: December 21, 1993Assignee: Farmitalia Carlo Erba s.r.l.Inventors: Piero Melloni, Philippe Dostert, Arturo D. Torre, Alberto Bonsignori
-
Patent number: 5264577Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.Type: GrantFiled: April 22, 1992Date of Patent: November 23, 1993Assignee: Warner-Lambert CompanyInventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, Mark E. Marlatt, John G. Topliss
-
Patent number: 5250722Abstract: The preparation of new 3,11-cyclotaxanes having the general formula 1. Cyclotaxane 1a (1, R'.dbd.R".dbd.H) may be isolated from plants of the genus Taxus. New cyclotaxanes 1 have antiblastic activity.Type: GrantFiled: May 11, 1992Date of Patent: October 5, 1993Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Bruno Gabetta
-
Patent number: 5245028Abstract: Processes for the preparation of a series of tetracyclic amines useful in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: September 3, 1991Date of Patent: September 14, 1993Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
-
Patent number: 5225586Abstract: The invention relates to benzocyclobutene capped benzotrifluoride based fluoroaryl ether compounds which are useful in preparing semi-permeable membranes, and films and coatings useful in electronic applications.Type: GrantFiled: September 13, 1991Date of Patent: July 6, 1993Assignee: The Dow Chemical CompanyInventors: Theodore L. Parker, Thomas W. Regulski
-
Patent number: 5220063Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.Type: GrantFiled: May 10, 1991Date of Patent: June 15, 1993Assignee: Hoechst Celanese CorporationInventors: Ahmed M. Tafesh, Olan S. Fruchey, Charles B. Hilton
-
Patent number: 5196454Abstract: The invention relates to novel 2,5-diaminotetralines of the formula: ##STR1## wherein R1, R2, R3 and R4 are defined herein, processes for preparing them and their use in pharmaceutical compositions. The novel 2,5-diaminotetralines are useful in treating diseases caused by disorders of the dopaminergic systems.Type: GrantFiled: June 15, 1990Date of Patent: March 23, 1993Assignee: Boehringer Ingelheim KGInventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
-
Patent number: 5187290Abstract: Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: September 29, 1986Date of Patent: February 16, 1993Assignee: E. R. Squibb & Sons, Inc.Inventor: Eric M. Gordon
-
Patent number: 5182303Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.Type: GrantFiled: May 20, 1991Date of Patent: January 26, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: John P. Daub, George P. Lahm, Bradford S. Marlin
-
Patent number: 5169952Abstract: An efficient process for stereoselective preparation of a medicinally significant hydroxyamide compound of structural formula: ##STR1## comprises the addition of metalated amide enolates to chiral .alpha.-amino metalated epoxides. The hydroxyamide reaction products are useful as inhibitors of the HIV protease or of renin, or as intermediates in the preparation of inhibitors of the HIV protease or renin.Type: GrantFiled: July 2, 1991Date of Patent: December 8, 1992Assignee: Merck & Co., Inc.Inventors: David Askin, Ralph Volante, Michael Wallace, Ichiro Shinkai
-
Patent number: 5153227Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.Type: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
-
Patent number: 5142094Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds are carbamates represented by the general formula ##STR1## wherein Ar and Ar' represent phenyl, naphthyl or heteroaryl, each of which may be substituted; Z and W are hydrogen, aliphatic hydrocarbon, heterocyclic, aryl or carbocyclic containing groups.Type: GrantFiled: September 18, 1990Date of Patent: August 25, 1992Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic
-
Patent number: 5140044Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.Type: GrantFiled: March 27, 1990Date of Patent: August 18, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
-
Patent number: 5130464Abstract: A method of manufacturing aromatic urethanes utilizes a urea production process wherein a primary aromatic amine, an aromatic nitro-compound and carbon monoxide are made to react together in the presence of a catalyst and solvents, to produce N,N'-disubstituted urea, the solvlent used in the urea production process consisting at least partly of an amide or oxygen-containing sulfur compound, and having the functions of stabilizing the catalyst and preventing it from separating out in a solution, and of increasing the activity of the catalyst, the quantity of the solvent being sufficient to permit it to fulfill these functions effectively. The method additionally includes an aromatic urethane production process wherein the N,N'-disubstituted urea produced is made to react with an organic compound containing hydroxyl groups, to produce a primary aromatic amine and aromatic urethane, the primary aromatic amine being separated to obtain the aromatic urethane.Type: GrantFiled: March 16, 1990Date of Patent: July 14, 1992Assignee: NKK CorporationInventors: Takao Ikariya, Masanori Itagaki, Mikoto Iemoto, Masatsugu Mizuguchi, Tetsuo Hachiya, Tomomichi Nakamura, Makoto Miyazawa, Sachiko Yamamoto
-
Patent number: 5126476Abstract: A process for making aryl-, heteroaryl-, or cycloalkyl-substituted alkyl urethanes is disclosed. The urethanes are prepared by electrophilic carbamylation of aromatic compounds with alkylene bis(carbamic acid esters) or the equivalent in the presence of an acidic catalyst and a polar aprotic solvent. The alkyl urethanes may be cracked to give the corresponding substituted alkyl isocyanates.Type: GrantFiled: January 25, 1991Date of Patent: June 30, 1992Assignee: Arco Chemical Technology, L.P.Inventors: Mahmoud K. Faraj, Haven S. Kesling, Jr., John G. Zajacek
-
Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
-
Patent number: 5109136Abstract: A novel series of tetracyclic amines, methods of preparation, compositions containing the amines, and methods for using them in the treatment and/or prevention of cerebrovascular disorders are disclosed.Type: GrantFiled: August 9, 1990Date of Patent: April 28, 1992Assignee: Warner-Lambert CompanyInventor: Thomas C. Malone
-
Patent number: 5101062Abstract: A process for producing carbamic acid esters (N-phenyl carbamate) which comprises reacting an amino group-containing compound (aniline), oxygen, a nitro group-containing compound (nitrobenzene), a carbon monoxide-containing gas and a hydroxyl group-containing organic compound (ethyl alcohol) in the presence of a compound of a transition metal belonging to Pt group of VIII group (Pd) of the Periodic Table as catalyst, a non-metal halide (HCl) and water.Type: GrantFiled: September 12, 1989Date of Patent: March 31, 1992Assignee: Babcock-Hitachi Kabushiki KaishaInventors: Mutsuo Yamada, Kazumi Murakami, Yasuyuki Nishimura, Fumito Nakajima, Nobuo Matsuo
-
Patent number: 5075490Abstract: New compounds N-.alpha.-9-fluorenylmethoxycarbonyl-aspartic acid-.beta.-1-adamantyl esters are stable under the basic condition of the normal peptide condensation process and do not form succinimide. Peptides containing aspartic acid can be synthesized with high purity and at high yields by using N-.alpha.-9-fluorenylmethoxycarbonyl-aspartic acid-.beta.-1-adamantyl ester.Type: GrantFiled: September 8, 1988Date of Patent: December 24, 1991Assignee: Watanabe Chemical Industries, Ltd.Inventor: Yoshio Okada
-
Patent number: 5057610Abstract: Substituted amino carbamate derivatives corresponding to the formula ##STR1## are effective in stabilizing organic materials against oxidative, thermal and actinic degradation, said derivatives being particularly effective as color improvers and process stabilizers in organic materials containing phenolic antioxidants and/or metal salts of fatty acids and/or hindered amine light stabilizers and/or organic phosphorus compounds; and certain of said derivatives as new compounds.Type: GrantFiled: April 25, 1988Date of Patent: October 15, 1991Assignee: Ciba-Geigy CorporationInventors: Stephen D. Pastor, Edward T. Hessell, Ramanathan Ravichandran
-
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: 5041606Abstract: A process for the preparation of a compound of formula ##STR1## wherein X represents hydrogen, halogen, trifluoromethyl or lower alkyl group; W represents methyl, Q represents hydrogen or W and Q, together, form an ethylene group and R' represents a lower alkyl group which comprises protecting the amino group of the phenol corresponding to the compound of formula I, submitting the compound thus obtained to an alkylation (with a compound of formula Hal--CH.sub.2 --COOR', wherein R' is as defined hereinabove for the formula I and Hal is chlorine, bromine or iodine) and then releasing the amino group of the product thus obtained.Type: GrantFiled: March 5, 1990Date of Patent: August 20, 1991Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
-
Patent number: 5024994Abstract: The invention concerns novel renin-inhibitory peptides which are useful for treating renin-assocated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.Type: GrantFiled: August 17, 1988Date of Patent: June 18, 1991Assignee: Warner-Lambert CompanyInventors: Annette M. Doherty, James P. Hudspeth, James S. Kaltenbronn, Joseph T. Repine, William H. Roark, Ila Sircar, Francis J. Tinney
-
Patent number: 5015644Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.Type: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi
-
Patent number: 5010105Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: May 9, 1990Date of Patent: April 23, 1991Assignee: Merck & Co., Inc.Inventor: Ta J. Lee
-
Patent number: 5008435Abstract: Process for producing urethanes, by reacting an organic hydroxyl group containing compound and carbon monoxide, either (i) with an organic nitro group containing compound, e.g. nitrobenzene, or (ii) with a primary amine, e.g. aniline, and oxygen, the reacting in both cases being carried out in the presence of a non-noble metal catalyst system comprising a copper catalyst, preferably mixed with a promoter such as a nitrogen or phosphorous containing organic compound for the (i) nitro compound reaction, or an alkali salt for the (ii) amine reaction, e.g. at 200-8000 psig and 100.degree.-300.degree. C., using 0.05-0.4 mole copper catalyst and 0.01-10 moles promoter per mole (i) nitro compound or (ii) amine, and 2-500 moles carbon monoxide, and (in the case of the (ii) amine) 0.5-5 moles oxygen, per mole of the (i) nitro compound or (ii) amine.Type: GrantFiled: November 22, 1988Date of Patent: April 16, 1991Assignee: Industrial Technology Research InstituteInventors: Kuo-Liang Loh, Puh Shieh, Y. S. Chao, Tsu-Kung Chuang
-
Patent number: 4987130Abstract: Substituted amino derivatives represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each stand for an acyclic hydrocarbon residue or an alicyclic hydrocarbon residue; R.sup.3 and R.sup.4 each stand for hydrogen or a hydrocarbon residue optionally containing hetero-atom(s); A stands for a carbon chain having two or more carbon atoms optionally containing ether linkage or sulfide linkage, which may be substituted and which may per se form a ring; X.sup.1 and X.sup.2 each stand for oxygen atom or sulfur atom; and Y stands for amino group or an organic residue bonded through nitrogen atom, which may form a ring by combining with a carbon atom constituting A; and their salts have anti-arrhythmic activity and are useful for prevention and treatment of a variety of arrhythmias.Type: GrantFiled: December 22, 1989Date of Patent: January 22, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Tsushima, Muneo Takatani, Minoru Hirata
-
Patent number: 4981865Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxygenase.Type: GrantFiled: May 26, 1989Date of Patent: January 1, 1991Assignee: Warner-Lambert Co.Inventors: Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
-
Patent number: 4975444Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.Type: GrantFiled: August 25, 1989Date of Patent: December 4, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
-
Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
-
Patent number: 4962224Abstract: Disclosed herein are N-naphthoylglycines and methods of their preparation. The N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: August 22, 1989Date of Patent: October 9, 1990Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Kazimir Sestanj
-
Patent number: 4960792Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James
-
Patent number: 4948913Abstract: A series of novel polypeptide derivatives, containing 5-amino-2,5-disubstituted-4-hydroxypentanoic acid residues, which are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin. Particularly valuable precursors for many of these compounds are certain other 5-amino-2,5-disubstituted-4-hydroxypentanoic acid derivatives.Type: GrantFiled: November 2, 1987Date of Patent: August 14, 1990Assignee: Pfizer Inc.Inventors: Edward F. Kleinman, Robert L. Rosati, Jasjit S. Bindra
-
Patent number: 4939169Abstract: Novel 1,4-naphthalenediol and 1,4-hydroquinone derivatives of formula I, II, III and IV and their therapeutic uses as 5-lipoxygenase inhibitors, leukotriene inhibitors, antiinflammatory and/or inhibitors of mucus secretion agents are described. Also provided are novel intermediates useful for the preparation of said derivatives.Type: GrantFiled: March 13, 1989Date of Patent: July 3, 1990Assignee: The Upjohn CompanyInventors: Gordon L. Bundy, Chiu-Hong Lin
-
Patent number: 4927955Abstract: A process for the preparation of a compound of formula ##STR1## wherein X represents hydrogen, halogen, trifluoromethyl or lower alkyl group; W represents methyl, Q represents hydrogen or W and Q, together, form an ethylene group and R' represents a lower alkyl group which comprises protecting the amino group of the phenol corresponding to the compound of formula I, submitting the compound thus obtained to an alkylation (with a compound of formula Hal--CH.sub.2 --COOR', wherein R' is as defined hereinabove for the formula I and Hal is chlorine, bromine or iodine) and then releasing the amino group of the product thus obtained.Type: GrantFiled: August 11, 1988Date of Patent: May 22, 1990Assignee: SanofiInventors: Robert Boigegrain, Roberto Cecchi, Sergio Boveri
-
Patent number: 4925968Abstract: Disclosed herein are N-acyl-N-naphthoylglycines and methods of their preparation. The N-acyl-N-naphthoylglycines are novel aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.Type: GrantFiled: January 9, 1989Date of Patent: May 15, 1990Assignee: American Home Products CorporationInventors: Kazimir Sestanj, Jay E. Wrobel, Joseph M. Kelly
-
Patent number: RE34137Abstract: The present invention relates to a method of manufacturing aromatic urethane, an aromatic mononitro-compound, an aromatic primary amine, and carbon monoxide being reacted using a catalyst containing a platinum group metal-containing compound as a major constituent to prepare N,N'-di-substituted urea. The resultant N,N'-di-substituted urea is reacted with a hydroxyl group-containing organic compound to prepare an aromatic primary amine and aromatic urethane, and the aromatic primary amine is separated to obtain aromatic urethane.Type: GrantFiled: October 12, 1989Date of Patent: December 1, 1992Assignee: NKK CorporationInventors: Takao Ikariya, Masanori Itagaki, Masatsugu Mizuguchi, Itaru Sakai, Osamu Tajima