Ring In Alcohol Moiety Patents (Class 560/32)
  • Patent number: 5189197
    Abstract: 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: Grant
    Filed: February 27, 1990
    Date of Patent: February 23, 1993
    Assignee: Shell Internationale Research Maatschappij B.V.
    Inventors: Pieter A. Verbrugge, Jannetje De Waal
  • Patent number: 5187270
    Abstract: 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: Grant
    Filed: January 6, 1989
    Date of Patent: February 16, 1993
    Assignee: Millipore Corporation
    Inventor: Michael S. Bernatowicz
  • Patent number: 5187290
    Abstract: 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: Grant
    Filed: September 29, 1986
    Date of Patent: February 16, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Eric M. Gordon
  • Patent number: 5176914
    Abstract: 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: Grant
    Filed: August 15, 1990
    Date of Patent: January 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd-Wieland Kruger, Klaus Sasse, Wilhelm Brandes
  • Patent number: 5166398
    Abstract: 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: Grant
    Filed: June 21, 1991
    Date of Patent: November 24, 1992
    Assignee: Warner-Lambert Co.
    Inventor: Paul L. Creger
  • Patent number: 5162311
    Abstract: 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: Grant
    Filed: August 19, 1991
    Date of Patent: November 10, 1992
    Assignee: Sandoz Pharmaceuticals Corp.
    Inventors: Paul L. Herrling, Werner Muller
  • Patent number: 5157143
    Abstract: 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: Grant
    Filed: May 11, 1989
    Date of Patent: October 20, 1992
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Dario Chiarino, Angelo Carenzi
  • Patent number: 5151414
    Abstract: 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: Grant
    Filed: July 31, 1991
    Date of Patent: September 29, 1992
    Assignee: SIMES Societa Italiana Medicinali e Sintetici S.p.A.
    Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
  • Patent number: 5142094
    Abstract: 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: Grant
    Filed: September 18, 1990
    Date of Patent: August 25, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic
  • Patent number: 5140044
    Abstract: 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: Grant
    Filed: March 27, 1990
    Date of Patent: August 18, 1992
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Teruo Kishi, Hiromitsu Saito, Hiroshi Sano, Isami Takahashi, Tatsuya Tamaoki
  • Patent number: 5134161
    Abstract: 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: Grant
    Filed: April 15, 1988
    Date of Patent: July 28, 1992
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Michael C. Venuti, John M. Young
  • Patent number: 5132312
    Abstract: 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: Grant
    Filed: November 27, 1990
    Date of Patent: July 21, 1992
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: John R. Regan, Kent E. Neuenschwander
  • Patent number: 5130464
    Abstract: 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: Grant
    Filed: March 16, 1990
    Date of Patent: July 14, 1992
    Assignee: NKK Corporation
    Inventors: Takao Ikariya, Masanori Itagaki, Mikoto Iemoto, Masatsugu Mizuguchi, Tetsuo Hachiya, Tomomichi Nakamura, Makoto Miyazawa, Sachiko Yamamoto
  • Patent number: 5130306
    Abstract: 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: Grant
    Filed: June 6, 1990
    Date of Patent: July 14, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 5126476
    Abstract: 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: Grant
    Filed: January 25, 1991
    Date of Patent: June 30, 1992
    Assignee: Arco Chemical Technology, L.P.
    Inventors: Mahmoud K. Faraj, Haven S. Kesling, Jr., John G. Zajacek
  • Patent number: 5124455
    Abstract: 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: Grant
    Filed: August 8, 1990
    Date of Patent: June 23, 1992
    Assignee: American Home Products Corporation
    Inventor: Louis J. Lombardo
  • Patent number: 5122539
    Abstract: 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: Grant
    Filed: May 20, 1991
    Date of Patent: June 16, 1992
    Assignee: Center for Innovative Technology
    Inventors: Donald J. Abraham, Mona Mahran, Ahmed Mehanna, Ramnarayan Randad
  • Patent number: 5118831
    Abstract: 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: Grant
    Filed: February 27, 1991
    Date of Patent: June 2, 1992
    Assignee: Ajinomoto Co., Inc.
    Inventors: Shigeo Nozoe, Tomihisa Ohta
  • Patent number: 5117057
    Abstract: 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: Grant
    Filed: June 14, 1991
    Date of Patent: May 26, 1992
    Assignee: Rohm and Haas Company
    Inventors: Adam C. Hsu, Harold E. Aller, Raymond A. Murphy, Dat P. Le, Donald W. Hamp, Barry Weinstein
  • Patent number: 5117031
    Abstract: 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: Grant
    Filed: June 20, 1989
    Date of Patent: May 26, 1992
    Assignee: Sanshin Kagaku Kogyo Co. Ltd.
    Inventor: Katsushige Kouge
  • Patent number: 5112859
    Abstract: 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: Grant
    Filed: September 14, 1990
    Date of Patent: May 12, 1992
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
  • Patent number: 5112868
    Abstract: 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: Grant
    Filed: May 2, 1990
    Date of Patent: May 12, 1992
    Assignee: Warner-Lambert Company
    Inventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
  • Patent number: 5108489
    Abstract: 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: Grant
    Filed: July 24, 1991
    Date of Patent: April 28, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 5102911
    Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.
    Type: Grant
    Filed: July 6, 1990
    Date of Patent: April 7, 1992
    Assignee: Merck & Co, Inc.
    Inventors: Ta J. Lee, Wilbur J. Holtz
  • Patent number: 5101059
    Abstract: 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: Grant
    Filed: December 5, 1989
    Date of Patent: March 31, 1992
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Louis A. Carpino, An-Chuu Wu
  • Patent number: 5099059
    Abstract: 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: Grant
    Filed: August 20, 1990
    Date of Patent: March 24, 1992
    Inventor: Don R. Baker
  • Patent number: 5087727
    Abstract: 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: Grant
    Filed: October 30, 1990
    Date of Patent: February 11, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Schrott, Peter Neumann, Michael Schmitt, Sibylle Brosius, Klaus D. Schomann, Harald Kuppelmaier
  • Patent number: 5081284
    Abstract: 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: Grant
    Filed: June 29, 1989
    Date of Patent: January 14, 1992
    Assignee: Suntory Limited
    Inventors: Naoki Higuchi, Masayuki Saitoh, Norio Iwasawa, Motoo Sumida, Hiroshi Shibata
  • Patent number: 5079383
    Abstract: 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: Grant
    Filed: July 25, 1990
    Date of Patent: January 7, 1992
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Fujihisa Matsunaga, Mitsuki Yasuhara
  • Patent number: 5077309
    Abstract: 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: Grant
    Filed: March 28, 1990
    Date of Patent: December 31, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 5070106
    Abstract: 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: Grant
    Filed: February 22, 1991
    Date of Patent: December 3, 1991
    Assignee: Simes Societa Italiana Medicinali e Sintetici S.p.A.
    Inventors: Cesare Casagrande, Gabriele Norcini, Francesco Santangelo, Claudio Semeraro
  • Patent number: 5055577
    Abstract: 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: Grant
    Filed: June 18, 1990
    Date of Patent: October 8, 1991
    Assignee: Monsanto Company
    Inventors: Dennis P. Riley, William D. McGhee
  • Patent number: 5049695
    Abstract: Allosteric hemoglobin modifier compounds having the general formula ##STR1## wherein X and Z may be CH.sub.2, NH or O.
    Type: Grant
    Filed: February 12, 1990
    Date of Patent: September 17, 1991
    Assignees: Center for Innovative Technology, Virginia Commonwealth University
    Inventors: Donald J. Abraham, Ahmed Mehanna, Ramnarayan Randad, Mona Mahran
  • Patent number: 5047420
    Abstract: 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: Grant
    Filed: August 21, 1989
    Date of Patent: September 10, 1991
    Assignee: 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
  • Patent number: 5021453
    Abstract: Compounds of formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: June 6, 1990
    Date of Patent: June 4, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Henry Joshua, Kenneth E. Wilson, Michael S. Schwartz, Ta J. Lee, Gerald E. Stokker
  • Patent number: 5015744
    Abstract: 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: Grant
    Filed: November 14, 1989
    Date of Patent: May 14, 1991
    Assignee: Florida State University
    Inventor: Robert A. Holton
  • Patent number: 5015644
    Abstract: 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: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 5011976
    Abstract: 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: Grant
    Filed: July 6, 1990
    Date of Patent: April 30, 1991
    Assignee: The Upjohn Company
    Inventor: Peter G. M. Wuts
  • Patent number: 5010105
    Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 23, 1991
    Assignee: Merck & Co., Inc.
    Inventor: Ta J. Lee
  • Patent number: 5010104
    Abstract: 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: Grant
    Filed: June 29, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5008435
    Abstract: 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: Grant
    Filed: November 22, 1988
    Date of Patent: April 16, 1991
    Assignee: Industrial Technology Research Institute
    Inventors: Kuo-Liang Loh, Puh Shieh, Y. S. Chao, Tsu-Kung Chuang
  • Patent number: 5004817
    Abstract: 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: Grant
    Filed: February 27, 1989
    Date of Patent: April 2, 1991
    Assignee: Montefibre, S.p.A.
    Inventors: Catia Bastioli, Salvatore Garlisi, Dario Fornara, Vittorio Bellotti
  • Patent number: 5001148
    Abstract: 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: Grant
    Filed: June 7, 1989
    Date of Patent: March 19, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Patent number: 4996201
    Abstract: 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: Grant
    Filed: August 2, 1989
    Date of Patent: February 26, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Stephen C. Bergmeier, Jeffrey A. Kester, Walter H. Moos, Haile Tecle, Anthony J. Thomas
  • Patent number: 4987248
    Abstract: 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: Grant
    Filed: August 2, 1989
    Date of Patent: January 22, 1991
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Francis J. Waller
  • Patent number: 4985180
    Abstract: 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: Grant
    Filed: June 6, 1989
    Date of Patent: January 15, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Harold E. Bellis, Donald J. Dumas, George C. Sonnichsen, Vinayakam Subramanyam
  • Patent number: 4960881
    Abstract: 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: Grant
    Filed: June 6, 1988
    Date of Patent: October 2, 1990
    Assignee: Societe Nationale des Poudres et Explosifs
    Inventors: Gerard Barcelo, Jean-Pierre Senet, Gerard Sennyey
  • Patent number: 4948807
    Abstract: 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: Grant
    Filed: March 8, 1989
    Date of Patent: August 14, 1990
    Assignee: Proterra AG
    Inventors: Marta W. Rosin, Michael Chorev, Zeev Tashma
  • Patent number: 4946863
    Abstract: 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: Grant
    Filed: January 18, 1989
    Date of Patent: August 7, 1990
    Assignee: H. Lundbeck A/S
    Inventors: Klaus P. Boegesoe, Jens K. Perregaard
  • Patent number: RE34137
    Abstract: 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: Grant
    Filed: October 12, 1989
    Date of Patent: December 1, 1992
    Assignee: NKK Corporation
    Inventors: Takao Ikariya, Masanori Itagaki, Masatsugu Mizuguchi, Itaru Sakai, Osamu Tajima