Ring In Alcohol Moiety Patents (Class 560/32)
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Patent number: 5189197Abstract: The invention provides a process for the preparation of N-benzoylcarbamates of general formula ##STR1## wherein R.sup.1 represents a hydrogen atom, a halogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group or a trifluoromethyl group, R.sup.2 represents a halogen atom, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group or a trifluoromethyl group, R.sup.3 represents a hydrogen atom, a halogen atom, a methyl group or a trifluoromethyl group, and R represents a C.sub.1-8 alkyl group optionally substituted by one or more halogen atoms or a phenyl group optionally substituted by one or more substituents selected from halogen atoms and methyl groups, characterized by reacting an alkali metal salt of a benzamide of general formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.Type: GrantFiled: February 27, 1990Date of Patent: February 23, 1993Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Pieter A. Verbrugge, Jannetje De Waal
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Patent number: 5187270Abstract: This invention pertains to amino acids attached to a solid support in a racemization free manner and to a method of covalently linking amino acids to solid supports for use in solid phase peptide syntheses.Type: GrantFiled: January 6, 1989Date of Patent: February 16, 1993Assignee: Millipore CorporationInventor: Michael S. Bernatowicz
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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
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Patent number: 5176914Abstract: Fungicidal carbocyclic anilide carbamates of the formula ##STR1## in which X represents optionally alkyl-substituted cycloalkyl or optionally alkyl-substituted cycloalkenyl,Hal represents halogen, andY.sup.1, Y.sup.2 and Y.sup.3 independently of one another represent hydrogen, halogen, optionally halogen-substituted alkyl, optionally halogen-substituted alkoxy or optionally halogen-substituted alkylthio, andR.sup.1 represents optionally halogen-substituted alkyl, alkenyl, alkylcarbonyloxyalkyl, alkenylcarbonyloxyalkyl and optionally substituted cycloalkyl which can be interrupted by hetero atoms, or represents optionally substituted phenyl or optionally substituted phenylalkyl, or R.sup.1 additionally can represent alkoxyalkyl, alkylthioalkyl or polyalkoxyalkyl if X represents optionally alkyl-substituted cycloalkenyl.Type: GrantFiled: August 15, 1990Date of Patent: January 5, 1993Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Klaus Sasse, Wilhelm Brandes
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Patent number: 5166398Abstract: Novel 4-oxy substituted phenoxyalkyl carboxylic acid, ester and alcohol derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: June 21, 1991Date of Patent: November 24, 1992Assignee: Warner-Lambert Co.Inventor: Paul L. Creger
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Patent number: 5162311Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.Type: GrantFiled: August 19, 1991Date of Patent: November 10, 1992Assignee: Sandoz Pharmaceuticals Corp.Inventors: Paul L. Herrling, Werner Muller
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Patent number: 5157143Abstract: A diastereoselective process for the preparation of compounds of formula ##STR1## (wherein R and R.sub.1 have the meanings reported in the specification and the asterisks show the asymmetric carbon atoms) starting from the corresponding N-protected 2-amino-3-aryl-propan-1-ol is described.The compounds of formula I are intermediates useful for the synthesis of pharmacologically active peptides.Type: GrantFiled: May 11, 1989Date of Patent: October 20, 1992Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Dario Chiarino, Angelo Carenzi
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Patent number: 5151414Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.Type: GrantFiled: July 31, 1991Date of Patent: September 29, 1992Assignee: SIMES Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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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
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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
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Patent number: 5134161Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;both X groups are the same and X is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6, whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.Type: GrantFiled: April 15, 1988Date of Patent: July 28, 1992Assignee: Syntex (U.S.A.) Inc.Inventors: Michael C. Venuti, John M. Young
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Patent number: 5132312Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.Type: GrantFiled: November 27, 1990Date of Patent: July 21, 1992Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John R. Regan, Kent E. Neuenschwander
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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
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Patent number: 5130306Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.Type: GrantFiled: June 6, 1990Date of Patent: July 14, 1992Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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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
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Patent number: 5124455Abstract: There are disclosed compounds of the formula ##STR1## wherein R is ##STR2## R.sup.1 is hydrogen, lower alkyl or ##STR3## a is 1-3; b is 1-3;c is 0-2;X, Y and Z are each, independently, a bond, O, S. or NH, with the proviso that if one of X or Y is O, S or NH, the other must be a bond;R.sup.2 is amino, loweralkylamino, arylamino, loweralkoxy or aryloxy;R.sup.3 is hydrogen, halo, hydroxy, lower alkoxy, aryloxy, loweralkanoyloxy, amino, lower alkylamino, arylamino or loweralkanoylamino;R.sup.4 and R.sup.5 are each, independently hydrogen or lower alkyl;m is 0-4;n is 1-4; ando is 1-4;and, which by virtue of their ability to selectively inhibit an isoenzyme of 3':5'-cyclic AMP phosphodiesterase located in pulmonary smooth muscle tissue and inflammatory cells, are bronchodilatory and antinflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.Type: GrantFiled: August 8, 1990Date of Patent: June 23, 1992Assignee: American Home Products CorporationInventor: Louis J. Lombardo
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Patent number: 5122539Abstract: Compounds of the general structural formula: ##STR1## wherein X, Y and Z may each be CH.sub.2, NH, or O, R.sub.2-6 are either hydrogen, halogen, or a substituted or unsubstituted C.sub.1, C.sub.2, or C.sub.3 alkyl group and these moieties maybe the same or different, or alkyl moieties of aliphatic or aromatic rings incorporating two of the R.sub.2-6 sites, R.sub.7-8 are hydrogen, methyl, or ethyl groups and these moieties may be the same or different, or alkyl moieties as part of an aliphatic ring connecting R.sub.7 and R.sub.8, and R.sub.9 is a hydrogen, loweralkyl such as methyl, ethyl or propyl, or a salt cation such as sodium, potassium, or ammonium are useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: May 20, 1991Date of Patent: June 16, 1992Assignee: Center for Innovative TechnologyInventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad
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Patent number: 5118831Abstract: Novel amino acid derivatives of the formula ##STR1## wherein R.sup.1 is a protecting group removable under reducing or acid conditions, and R.sup.2 and R.sup.5 are hydrogen or carboxylic protecting groups, are useful as intermediates in preparing stereospecific carbapenam/carbapenem derivatives. R.sup.1 is removed under reducing conditions to form a pyrrolidine derivative, which is further cyclized from the R.sup.5 .dbd.H compound to form a .beta.-lactam ring. Stereospecificity at the 6-position is achieved by treatment with lithium diisopropylamide (LDA) and quenching at different temperatures. Compound (I) can be prepared by treating R.sup.1 -protected R.sup.3 -pyrrolidone carboxylic acid R.sup.2 -ester with a lithium enolate of the formula R.sup.4 CHLiCO.sub.2 R.sup.5. The lithium enolate can be formed from R.sup.4 CH.sub.2 CO.sub.2 R.sup.5 by treatment with LDA.Type: GrantFiled: February 27, 1991Date of Patent: June 2, 1992Assignee: Ajinomoto Co., Inc.Inventors: Shigeo Nozoe, Tomihisa Ohta
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Patent number: 5117057Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-disubstitutedhydrazines, methods of using such compositions and N'-substituted-N, N'-disubstitutedhydrazines. Specifically, the invention relates to insect growth regulating compositions, and methods of using such compositions, which include compounds having a nucleus of the formula ##STR1## where A', B', D and J are independently any atom or group of atoms; where E is a tertiary carbon containing organic radical, a haloalkyl having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen, and is attached to the nitrogen shown in the formula by a carbon-to-nitrogen single bond; where one G.sub.1 is C, N, O and S, and both G.sub.2 's and the other G.sub.1 are carbon; or one G.sub.2 is S or P, and both G.sub.1 's and the other G.sub.Type: GrantFiled: June 14, 1991Date of Patent: May 26, 1992Assignee: Rohm and Haas CompanyInventors: Adam C. Hsu, Harold E. Aller, Raymond A. Murphy, Dat P. Le, Donald W. Hamp, Barry Weinstein
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Patent number: 5117031Abstract: This invention is characterized by synthesizing an active ester represented by the general formula ##STR1## using an active esterifying agent consisting of a sulfonium salt represented by the general formula ##STR2## and further reacting the above-said active ester with a nucleophilic agent represented by the general formula H-B-Y to produce an ester or amide represented by the general formula (W) d.A-B-Y.Type: GrantFiled: June 20, 1989Date of Patent: May 26, 1992Assignee: Sanshin Kagaku Kogyo Co. Ltd.Inventor: Katsushige Kouge
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Patent number: 5112859Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.Type: GrantFiled: September 14, 1990Date of Patent: May 12, 1992Assignee: American Home Products CorporationInventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
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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
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Patent number: 5108489Abstract: Herbicidal disubstituted naphthalenes of the formula ##STR1## in which A represents optionally branched alkanediyl,R represents hydrogen or in each case optionally substituted alkyl or phenyl,R.sup.1 represents hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 represents hydrogen or halogen,R.sup.3 represents halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio or trifluoromethylsulphonyl,R.sup.4 represents hydrogen or halogen,X represents nitrogen or the group C--R.sup.5, whereR.sup.5 represents hydrogen or halogen,Y represents oxygen or sulphur, andZ represents oxygen, the group N--(O).sub.n --R.sup.Type: GrantFiled: July 24, 1991Date of Patent: April 28, 1992Assignee: Bayer AktiengesellschaftInventors: Roland Andree, Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5102911Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: July 6, 1990Date of Patent: April 7, 1992Assignee: Merck & Co, Inc.Inventors: Ta J. Lee, Wilbur J. Holtz
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Patent number: 5101059Abstract: This invention relates to compounds of the formula a compound of the formula ##STR1## wherein X is O, CR.sub.7 R.sub.8, S or NR.sub.9 wherein R.sub.7 and R.sub.8 are independently hydrogen, or lower alkyl, and R.sub.9 is lower alkyl;n is 0 or 1;R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, monoorganosilyl, diorganosilyl, triorganosilyl, halogen, aryl, or nitro;R.sub.3 is hydrogen, lower alkyl, monoorganosilyl, diorganosilyl, triorganosilyl, halogen, 9-fluorenylalkyl, cycloalkyl, aryl or aralkyl;R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or aryl or one of R.sub.4 and R.sub.5 is 9-fluorenyl;R.sub.6 is H or COZ wherein Z is an amino acid, a peptide residue or a leaving group; andwith the provisos that when n is 0 and R.sub.3 is hydrogen, R.sub.1 and R.sub.2 are not hydrogen, halogen or nitro; that when n is 0 and R.sub.3 is lower alkyl, R.sub.1 and R.sub.2 are not hydrogen; and that when X is O or CR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are H, that R.sub.1, R.sub.2, R.sub.Type: GrantFiled: December 5, 1989Date of Patent: March 31, 1992Assignee: Research Corporation Technologies, Inc.Inventors: Louis A. Carpino, An-Chuu Wu
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Patent number: 5099059Abstract: Substituted phenyl carbamates of the formula ##STR1## in which: R is a member selected from the group consisting of halogen, trifluoromethyl, cyano, NO.sub.2 and C.sub.1 -C.sub.3 haloalkyloxy;R.sub.1 is methyl or ethyl;R.sub.2 is independently selected from the group consisting of H, cyano, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.4 haloalkyl; andn is the number of R.sub.2 substituents other than hydrogen and equals 1-5;and their use as herbicides are disclosed herein.Type: GrantFiled: August 20, 1990Date of Patent: March 24, 1992Inventor: Don R. Baker
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Patent number: 5087727Abstract: Azulenesquaric acid dyes of the formula ##STR1## where L is substituted or unsubstituted C.sub.1 -C.sub.12 - alkylene,R.sup.1 is C.sub.1 -C.sub.20 - alkyl, C.sub.5 -C.sub.7 - cycloalkyl or substituted or unsubstituted phenyl andR.sup.2, R.sup.3, and R.sup.5 are each independently of the others hydrogen or substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl,with the proviso that when R.sup.5 is hydrogen the positions of the substituents CH.sub.2 --L--O--CO--NHR.sup.1 and R.sup.4 on an azulene ring may also be interchanged within a ring in either or both of the azulene rings, derived from azulene intermediates that contain urethane groups, are suitable for use in an optical recording medium.Type: GrantFiled: October 30, 1990Date of Patent: February 11, 1992Assignee: BASF AktiengesellschaftInventors: Wolfgang Schrott, Peter Neumann, Michael Schmitt, Sibylle Brosius, Klaus D. Schomann, Harald Kuppelmaier
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Patent number: 5081284Abstract: A novel N-substituted peptidyl compound represented by the general formula (1): ##STR1## where R.sub.1 is a straight-chained or branched acyl group having 2-10 carbon atoms, a branched, cyclic or partly branched cyclic alkyloxycarbonyl group having 4-15 carbon atoms, a substituted or unsubstituted benzyloxycarbonyl group, a 2,2,2-trichloroethyloxycarbonyl group, a 2-(trimethylsilyl)ethyloxycarbonyl group, a p-toluensulfonyl group, an o-nitrophenylsulfenyl group, a diphenylphosphonothioyl group, a triphenylmethyl group, a 2-benzoyl-1-methylvinyl group or a 4-phenylbutyryl group; R.sub.2 is a hydrogen atom or when taken together with R.sub.1, may form a phthaloyl group; R.sub.3 is an isobutyl group, a n-butyl group or an isopropyl group; R.sub.4 is a butyl group, a benzyl group or a methylthioethyl group; and R.sub.5 is a hydrogen atom or a chloromethyl group, which inhibits the activity of cysteine proteinases.Type: GrantFiled: June 29, 1989Date of Patent: January 14, 1992Assignee: Suntory LimitedInventors: Naoki Higuchi, Masayuki Saitoh, Norio Iwasawa, Motoo Sumida, Hiroshi Shibata
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Patent number: 5079383Abstract: A process for producing 4,4'-diphenylmethane dicarbamates through one-stage condensation by reacting N-phenyl carbamates with a methylenating agent in presence of a zinc halide, as a catalyst. 4,4'-diphenylmethane dicarbamates can be produced with high selectivity and in high yield.Type: GrantFiled: July 25, 1990Date of Patent: January 7, 1992Assignee: Mitsui Petrochemical Industries, Ltd.Inventors: Fujihisa Matsunaga, Mitsuki Yasuhara
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Patent number: 5077309Abstract: Novel compounds have the formula (I) ##STR1## where ##STR2## represents one of the divalent cyclic groups ##STR3## the letters a and b indicating in each case the points of attachment of the substituents R.sup.1 and CV(R.sup.2)-NV'R, respectively; R.sup.1 is a group --(CH.sub.2).sub.b --(A).sub.a --(CH.sub.2).sub.c --B--CH.sub.2 --CO.sub.2 R' in which A and B are each separately oxygen or sulphur, a is 0, b is 0 and c is an integer from 3 to 10, or a is 1, b is 0 or an integer from 1 to 7 and c is an integer from 2 to 9 with the sum of b and c being from 2 to 9, and CO.sub.2 R' is a carboxy group or an amide, ester or salt derivative thereof; V and V' either each separately is hydrogen or together are the second bond of a carbon-nitrogen double bond; R.sup.2 is hydrogen, an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by an aromatic group directly or through an oxygen or sulphur atom; and R is a group --OR.sup.3, --OR.sup.4, --D--R.sup.3, --N.dbd. R.sup.5 or --NW.G.Type: GrantFiled: March 28, 1990Date of Patent: December 31, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5070106Abstract: Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m, and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.Type: GrantFiled: February 22, 1991Date of Patent: December 3, 1991Assignee: Simes Societa Italiana Medicinali e Sintetici S.p.A.Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
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Patent number: 5055577Abstract: The present invention provides a process for preparing urethanes from primary or secondary amines, carbon dioxide and a diolefin. The amine is reacted with carbon dioxide to form the ammonium carbamate salt which is then reacted with a stoichiometric amount of a diolefin coordinated to palladium(II).Type: GrantFiled: June 18, 1990Date of Patent: October 8, 1991Assignee: Monsanto CompanyInventors: Dennis P. Riley, William D. McGhee
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Patent number: 5049695Abstract: Allosteric hemoglobin modifier compounds having the general formula ##STR1## wherein X and Z may be CH.sub.2, NH or O.Type: GrantFiled: February 12, 1990Date of Patent: September 17, 1991Assignees: Center for Innovative Technology, Virginia Commonwealth UniversityInventors: Donald J. Abraham, Ahmed Mehanna, Ramnarayan Randad, Mona Mahran
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 5021453Abstract: Compounds of formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: June 6, 1990Date of Patent: June 4, 1991Assignee: Merck & Co., Inc.Inventors: Henry Joshua, Kenneth E. Wilson, Michael S. Schwartz, Ta J. Lee, Gerald E. Stokker
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Patent number: 5015744Abstract: Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; the contacting of said alcohol and oxazinone being carried out in the presence of a sufficient amount of an activating agent under effective conditions to cause the oxazinone to react with the alcohol to form a .beta.-amido ester which is suitable for use as an intermediate in the synthesis of taxol.Type: GrantFiled: November 14, 1989Date of Patent: May 14, 1991Assignee: Florida State UniversityInventor: Robert A. Holton
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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
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Patent number: 5011976Abstract: An intermediate useful in the preparation of deferoxamine having Formula IX--Ph--CH.sub.2 --O--C(O)--NH--(CH.sub.2).sub.4 CH.dbd.NORwherein X is a C.sub.1 -C.sub.4 alkyl, --O(C.sub.1 -C.sub.4 alkyl), a halogen or hydrogen; R is X--Ph--CH.sub.2 -- or hydrogen. In one embodiment X and R are hydrogen. The intermediate has the advantage of being prepared in fewer and more efficient steps from readily available materials than conventional means for preparing deferoxamine.Type: GrantFiled: July 6, 1990Date of Patent: April 30, 1991Assignee: The Upjohn CompanyInventor: Peter G. M. Wuts
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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
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Patent number: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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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
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Patent number: 5004817Abstract: Compounds having the formula (I): ##STR1## wherein: M is an alkali or alkaline-earth metal or a C.sub.1 -C.sub.18 alkyl group;X is a group selected from --CH.sub.2 --, --CO--, --CH.sub.2 --CO--, --CH(CH.sub.3)--CO--,p is 0 or 1;Ar is a simple or condensed aromatic ring or Ar represents two or more aromatic nuclei bonded either by a simple bond or by an --O--, --S--, --SO.sub.2 --, --SO--, --CO--, --CS--, or --NH-- group;y is H or CH.sub.3 ;m is 1 when Y=--CH.sub.3, or an integer from 1 to 5 (including both values) when Y=H; n is a number ranging from 1 to 500 (including both values); andZ is H; a C.sub.1 -C.sub.18 alkyl; benzyl; glycidyl; acetyl; allyl; --CO--NH--R or --CO--NH--R.sub.1 --NCO group.Type: GrantFiled: February 27, 1989Date of Patent: April 2, 1991Assignee: Montefibre, S.p.A.Inventors: Catia Bastioli, Salvatore Garlisi, Dario Fornara, Vittorio Bellotti
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4996201Abstract: 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates 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: August 2, 1989Date of Patent: February 26, 1991Assignee: Warner-Lambert Co.Inventors: Stephen C. Bergmeier, Jeffrey A. Kester, Walter H. Moos, Haile Tecle, Anthony J. Thomas
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Patent number: 4987248Abstract: An improved for preparing N-substituted carbamate comprising reaction of a selected olefin or alcohol with a carbamate in the presence of a catalyst comprising a blend of a perfluorinated sulfonic acid polymer and a perfluorinated polymer diluent in a substantially nonpolar reaction mixture.Type: GrantFiled: August 2, 1989Date of Patent: January 22, 1991Assignee: E. I. du Pont de Nemours and CompanyInventor: Francis J. Waller
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Patent number: 4985180Abstract: Phenyl esters of substituted acids are prepared by a two-step process in which a phenol derivative is first treated with an acid halide to yield a phenyl ester intermediate, and the intermediate is reacted with an appropriate nucleophile.Type: GrantFiled: June 6, 1989Date of Patent: January 15, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Harold E. Bellis, Donald J. Dumas, George C. Sonnichsen, Vinayakam Subramanyam
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Patent number: 4960881Abstract: The invention relates to carbonates of formula: ##STR1## in which X is a fluorine, chlorine or bromine atom and R.sup.1 is different from the ##STR2## group and represents: a substituted or non-substituted, saturated or unsaturated, aliphatic, araliphatic, primary, secondary, tertiary or cycloaliphatic radical. These .alpha.-chlorinated carbonates are prepared by the action of a compound of formula R.sup.1 OH on a chloroformate of formula: ##STR3## in a solvent medium in the presence of an acid scavenger which is added after the two preceding compounds. They are used to block the amine function of amino acids. The .alpha.-chlorinated carbonate and amino acid are reacted in a solvent medium at a temperature of -5.degree. to 100.degree. C. in the presence of an acid scavenger. Blocked amines are very useful in peptide synthesis.Type: GrantFiled: June 6, 1988Date of Patent: October 2, 1990Assignee: Societe Nationale des Poudres et ExplosifsInventors: Gerard Barcelo, Jean-Pierre Senet, Gerard Sennyey
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Patent number: 4948807Abstract: Phenyl carbamates of the general formula ##STR1## wherein R.sub.1 to R.sub.5 are as defined in the claims, are useful as pharmaceuticals.Type: GrantFiled: March 8, 1989Date of Patent: August 14, 1990Assignee: Proterra AGInventors: Marta W. Rosin, Michael Chorev, Zeev Tashma
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Patent number: 4946863Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.Type: GrantFiled: January 18, 1989Date of Patent: August 7, 1990Assignee: H. Lundbeck A/SInventors: Klaus P. Boegesoe, Jens K. Perregaard
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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