Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/354)
  • Patent number: 6312738
    Abstract: A process of producing an azadirachtin-rich aqueous solution is disclosed which comprises de-oiling by pressing whole or ground neem seeds to remove a first proportion of the oil content; extracting the de-oiled neem seeds with a polar organic solvent in which the azadirachtin is soluble but in which polysaccharides and proteins are not substantially soluble; partitioning the organic solvent solution against water to form an aqueous solution of azadirachtin and the remaining oil; and separating the remaining oil from the azadirachtin-rich aqueous solution. Additional steps of the process are also disclosed.
    Type: Grant
    Filed: January 14, 2000
    Date of Patent: November 6, 2001
    Assignee: Neem Extracts Pty. Ltd.
    Inventors: Michael J. O'Shea, Donald J. Brushett, David J. Pollard
  • Patent number: 6307068
    Abstract: The invention relates to compound of the general formula (I): R—O—A  (I) wherein: R represents the radical of formula (II): A is as defined in the description, and medicinal products containing the same which are useful in treating or in preventing cancer.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: October 23, 2001
    Assignee: Adir et Compagnie
    Inventors: Ying Li, Feng Shan, Jin Ming Wu, Guangshao Wu, Jian Ding, Jianxian Han, Ghanem Atassi, Pierre Renard
  • Patent number: 6297260
    Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
    Type: Grant
    Filed: October 29, 1999
    Date of Patent: October 2, 2001
    Assignee: NitroMed, Inc.
    Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang
  • Patent number: 6271425
    Abstract: A novel process for producing alcohols, characterized by reacting an organic halide represented by the formula R—X (wherein R means an organic residue and X means a halogen atom) with oxygen molecules in the presence of an organotin compound and a reducing agent and optionally in the presence of a free-radical inhibitor in an amount up to 0.3 equivalent based on the organic halide to obtain an alcohol represented by the general formula R—OH (wherein R has the same meaning as the above).
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: August 7, 2001
    Assignees: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Eiichi Nakamura, Masaya Sawamura
  • Patent number: 6245806
    Abstract: Novel tetracyclic aromatic ketones are natural product compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. Further, the novel fungal cultures MF6388 (ATCC 74478), Sterile Fungus, and MF6591 (ATCC 74477), Ascochyta sp. are also disclosed. Further, the cultures Sterile Fungus MF6388 (ATCC 74478) and Ascochyta sp. MF6591 (ATCC 74477) are also disclosed, as well as processes for making compounds of the present invention employing the cultures.
    Type: Grant
    Filed: July 25, 2000
    Date of Patent: June 12, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Anne Dombrowski, Sheo Singh, Deborah L. Zink, Ana Teran, Fernando Pelaez, Daria Hazuda
  • Patent number: 6225338
    Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins-and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.
    Type: Grant
    Filed: October 15, 1998
    Date of Patent: May 1, 2001
    Assignee: Mars Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
  • Patent number: 6187543
    Abstract: The present invention relates, in general, to tristetraprolin (TTP) and, in particular, to methods of modulating levels of tumor necrosis factor &agr; (TNF&agr;) using TTP or nucleic acid sequences encoding same. The invention further relates to methods of screening for compounds for their ability to inhibit TNF&agr; biosynthesis.
    Type: Grant
    Filed: April 19, 1999
    Date of Patent: February 13, 2001
    Assignee: Duke University
    Inventor: Perry J. Blackshear
  • Patent number: 6156282
    Abstract: The invention relates to new calixarenes of formula: ##STR1## in which R.sup.1 represents a crown ether chain that includes at least two aryl or cycloalkyl rings,R.sup.2 is a hydroxyl or alkoxy group, or the two R.sup.2 groups together form a crown ether chain such as R.sup.1, and R.sup.3 represents a hydrogen atom or an alkyl group. The calixarenes are used to selectively extract caesium from aqueous solutions that notably have high concentrations of sodium.
    Type: Grant
    Filed: January 27, 1999
    Date of Patent: December 5, 2000
    Assignee: Commissariat a l'Energie Atomique
    Inventors: Jean-Fran.cedilla.ois Dozol, Veronique Lamare, Christophe Bressot, Rocco Ungaro, Alessandro Casnati, Jacques Vicens, Zouhair Asfari
  • Patent number: 6100293
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: August 8, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Shouwu Miao, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 6060468
    Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, p, r and s are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for treatment of indications caused by or related to secretion and circulation of insulin antagonising peptides.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 9, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
  • Patent number: 6057441
    Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereoisomeric forms thereof, wherein n is zero to 6; p and q are zero to 4; r is zero to 5; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; halomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or halomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: May 2, 2000
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
  • Patent number: 6054448
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,and R.sup.2, R.sup.3, R.sup.4, X and Z are as defined in the specification, possess affinity for metabotropic glutamate receptors and are useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: April 25, 2000
    Assignee: Eli Lilly and Company Limited
    Inventors: Barry Peter Clark, John Richard Harris
  • Patent number: 5990104
    Abstract: Polycyclic alkaloids of formula (I), wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6, or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X ix O, S, SO, SO.sub.2, or N--R.sub.5, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; and m is an integer from 0 to 3. These compounds act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.
    Type: Grant
    Filed: March 25, 1998
    Date of Patent: November 23, 1999
    Assignee: Biochem Pharma, Inc.
    Inventors: John Dimaio, Dilip M. Dixit
  • Patent number: 5948817
    Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.
    Type: Grant
    Filed: March 4, 1998
    Date of Patent: September 7, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventors: James Epperson, Graham Johnson, Daniel J. Keavy, Katherine S. Takaki
  • Patent number: 5926687
    Abstract: The invention relates to crown calix.vertline.4.vertline.arenes, their preparation process and their use for the selective extraction of cesium and actinides. These crown calixl4larenes comply with the formula: ##STR1## in which R.sub.1 represents a group of formula X(C.sub.2 H.sub.4 X).sub.m and X(C.sub.2 H.sub.4 X).sub.n YX(C.sub.2 H.sub.4 X).sub.n with X=O or N(R.sub.4), m=3, 4, 5 or 6, Y=cycloalkylene or arylene and n=1, 2 or 3. These crown.vertline.4.vertline.arenes, whose benzene nuclei are optionally substituted by alkyl groups, can be used as extractants, e.g. in liquid membrane form, for separating cesium from acid solutions containing sodium in a large quantity compared with the cesium quantity, e.g. irradiated fuel reprocessing plant effluents.
    Type: Grant
    Filed: October 4, 1995
    Date of Patent: July 20, 1999
    Assignee: Commissariat a l'Energie Atomique
    Inventors: Jean-Fran.cedilla.ois Dozol, Helene Rouquette, Rocco Ungaro, Alessandro Casnati
  • Patent number: 5917057
    Abstract: This invention relates to N-hydroxy-dibenz?b,e!oxepinalkylamines, N-hydroxy-dibenz?b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: June 29, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
  • Patent number: 5883119
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: March 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5843986
    Abstract: A compound selected from those of formula (I): ##STR1## in which A, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description, and a medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.
    Type: Grant
    Filed: October 19, 1995
    Date of Patent: December 1, 1998
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Hamid Ait Mansour, Philippe Delagrance, Pierre Renard
  • Patent number: 5840749
    Abstract: This invention relates to N-hydroxy-dibenz?b,e!oxepinalkylamines, N-hydroxy-dibenz?b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: November 24, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
  • Patent number: 5789496
    Abstract: A method for the removal, separation, and concentration of cesium cations from a source solution which may contain larger concentrations of other alkali metal ions comprises bringing the source solution into contact with a polymeric resin containing poly(hydroxyarylene) ligands. The poly(hydroxyarylene) ligand portion(s) of the polymeric resins has affinity for cesium, thereby removing cesium from the source solution. The source solutions from which the cesium has been removed may then be treated or disposed of as desired and the cesium cations are then removed from the polymeric resin through contact with a much smaller volume of a receiving solution in which these cesium cations are soluble and has greater affinity for such cations than does the poly(hydroxyarylene) ligand or protonates the ligand, thereby quantitatively stripping the completed cesium cations from the ligand and recovering them in concentrated form in said receiving solution.
    Type: Grant
    Filed: January 24, 1997
    Date of Patent: August 4, 1998
    Assignee: IBC Advanced Technologies, Inc.
    Inventors: Bryon J. Tarbet, Garren Maas, Krzysztof E. Krakowiak, Ronald L. Bruening
  • Patent number: 5780500
    Abstract: Base-substituted debenz?b,f!oxepines of formula I ##STR1## wherein alk is a divalent aliphatic radical, R is an amino group that is unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals or disubstituted by divalent aliphatic radicals, and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and pharmaceutically acceptable salts thereof, may be used as anti-neurodegenerative active ingredients of medicaments. The invention relates also to novel compounds of formula I.
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: July 14, 1998
    Assignee: Novartis Corporation
    Inventors: Claudia Betschart, Kaspar Zimmermann
  • Patent number: 5780501
    Abstract: Base-substituted dibenz?b,f!oxepines of formula I ##STR1## wherein alk is a divalent aliphatic radical, R is an amino group that is unsubstituted or mono- or di-substituted by monovalent aliphatic and/or araliphatic radicals or disubstituted by divalent aliphatic radicals, and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and pharmaceutically acceptable salts thereof, may be used as anti-neurodegenerative active ingredients of medicaments. The invention relates also to novel compounds of formula I.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: July 14, 1998
    Assignee: Novartis Corporation
    Inventors: Claudia Betschart, Kaspar Zimmermann
  • Patent number: 5773262
    Abstract: The present invention aims at enhancing purity of the proanthocyanidin extracts by acting yeast to the proanthocyanidin extracts for fermenting them to thereby assimilate the impurities such as saccharides with yeast to reduce them.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: June 30, 1998
    Assignee: Kikkoman Corporation
    Inventors: Toshiaki Ariga, Hiroshi Hosoyama, Katsumi Yuasa
  • Patent number: 5741814
    Abstract: Cyclooctadiene derivative of the following formula (1): ##STR1## wherein A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each independently represent COOR.sup.5 (where R.sup.5 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a phenyl group, a C.sub.7 -C.sub.12 aralkyl group or CONR.sup.6 R.sup.7 (where R.sup.6 and R.sup.7 each independently represent a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group), or A.sup.1 and A.sup.2, and/or A.sup.3 and A.sup.4 may be combined together to represent group(s) of: ##STR2## in which X represents an oxygen atom or NR.sup.8 {where R.sup.8 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group or a phenyl group),R.sup.0, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a halogen atom, a hydroxyl group and an C.sub.1 -C.sub.10 alkyl group,the symbol ------ represents a single or double bond, and when it is a double bond, then R.sup.1 and R.sup.
    Type: Grant
    Filed: September 3, 1996
    Date of Patent: April 21, 1998
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yasuyuki Nakajima, Hisayuki Watanabe, Michiaki Adachi, Michito Tagawa, Mitsugu Futagawa, Takashi Furusato, Hiroshi Ohya, Masanori Nishioka
  • Patent number: 5728727
    Abstract: A compound of Formula I, which is named {5R*-?6R*, 7S*, 8R*, 9R*, 12S*, 16S*, 18S*, 19S*, (13E)!} 4, 7, 19-trihydroxy-2, 6, 8, 12, 12, 14, 16, 18-heptamethyl-6, 7, 8, 9, 10, 11, 12, 15, 16, 17, 18, 19-dodecahydro-1, 19:5, 9-diepoxybenzocyclooctadecen-3 (5H)-one, and which is useful in inhibiting bone resorption, and treating and inhibiting osteoporosis.
    Type: Grant
    Filed: October 3, 1996
    Date of Patent: March 17, 1998
    Assignee: American Home Products Corporation
    Inventors: Michael H. Su, Margaret I. Hosken, Brian J. Hotovec, Terra L. Johnston
  • Patent number: 5726325
    Abstract: The present invention relates to tricyclic compounds represented by general formula (I) which are useful as therapeutic agents for urinary incontinence: ##STR1## wherein R.sup.1 represents hydrogen and the like; --X.sup.1 --X.sup.2 --X.sup.3 -- represents --CR.sup.2 .dbd.CR.sup.3 --CR.sup.4 .dbd.CR.sup.5 -- (wherein R.sup.2, R.sup.3, R.sup.4, and R.sup.5 represent hydrogen and the like) and the like; and Y represents --CH.sub.2 O-- and the like.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: March 10, 1998
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Makoto Yoshida, Shin-ichi Sasaki, Shigeru Aono, Shigeki Fujiwara, Haruki Takai, Tsuyoshi Yamagata, Ken Nagashima, Akira Karasawa
  • Patent number: 5726203
    Abstract: This invention relates to the compounds represented by general formula (I) and the processes for their preparation, wherein R is selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl unsubstituted or substituted by a halogen atom or nitro group, biphenyl unsubstituted by a halogen atom or nitro group, naphthyl unsubstituted or substituted by a halogen atom or nitro group. The compounds of this invention are used to prepare agents for prevention and treatment of AIDS and drugs against malaria and toxoplasmosis.
    Type: Grant
    Filed: May 21, 1996
    Date of Patent: March 10, 1998
    Inventors: Zelin Li, Xuande Luo, Yi Zeng, Lin Ma
  • Patent number: 5712305
    Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.
    Type: Grant
    Filed: July 26, 1996
    Date of Patent: January 27, 1998
    Assignee: MARS, Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
  • Patent number: 5695763
    Abstract: Azadirachtin is effectively recovered from the seeds of the neem tree by crushing the seeds, extracting azadirachtin from the crushed seeds with water and then either extracting azadirachtin from the water using a non-aqueous solvent which is not miscible with water and has a higher solubility of azadirachtin than water or a surfactant having a turbidity temperature between 20.degree. and 80.degree. C. The concentrated azadirachtin is easily recovered from the second extraction solution and shows high activity as an insecticide.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: December 9, 1997
    Assignee: Trifolio-M GmbH, Herstellung Und Vertrieb
    Inventor: Hubertus Kleeberg
  • Patent number: 5696156
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: December 9, 1997
    Assignee: Merck & Co. Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5679703
    Abstract: Disclosed is a tricyclic compound represented by formula (I): ##STR1## where X.sup.1 -X.sup.2 represents CH.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.N or S--CH.dbd.CH;Y--Z represents CH.sub.2 --O or CH.sub.2 --S; thenL--M represents C.dbd.CR.sup.9 (in which R.sup.9 represents hydrogen or lower alkyl) or CH--CR.sup.10 R.sup.11 (in which each of R.sup.10 and R.sup.11 independently represents hydrogen or lower alkyl);W represents NR.sup.4 (in which R.sup.4 represents hydrogen or lower alkyl) or O;each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen, lower alkyl, lower alkoxy, halogen, nitro, amino or mono or di-lower alkyl-substituted amino;R.sup.5 represents hydrogen or lower alkyl;each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, halogen, lower alkyl or lower alkoxy;provided that when Y--Z represents CH.dbd.CH or CH.sub.2 CH.sub.2, then L--M represents C.dbd.CR.sup.9 (in which R.sup.9 has the same meaning as defined above),or CH--CR.sup.10a R.sup.11a (in which each of R.sup.
    Type: Grant
    Filed: September 7, 1995
    Date of Patent: October 21, 1997
    Assignee: Kyowa Hakko Kogyo, Co., Ltd.
    Inventors: Masashi Yanase, Toshiaki Kumazawa, Shiro Shirakura, Eiko Oishi, Koji Yamada
  • Patent number: 5679705
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 16, 1996
    Date of Patent: October 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 5656702
    Abstract: A method for the removal separation, and concentration of cesium cations from a source solution which may contain larger concentrations of other alkali metal ions comprises bringing the source solution into contact with a polymeric resin containing poly(hydroxyarylene) ligands. The poly(hydroxyarylene) ligand portion(s) of the polymeric resins has affinity for cesium, thereby removing cesium from the source solution. The source solutions from which the cesium has been removed may then be treated or disposed of as desired and the cesium cations are then removed from the polymeric resin through contact with a much smaller volume of a receiving solution in which these cesium cations are soluble and has greater affinity for such cations than does the poly(hydroxyarylene) ligand or protonates the ligand, thereby quantitatively stripping the complexed cesium cations from the ligand and recovering them in concentrated form in said receiving solution.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: August 12, 1997
    Assignee: IBC Advanced Technologies, Inc.
    Inventors: Bryon J. Tarbet, Garren Maas, Krzysztof E. Krakowiak, Ronald L. Bruening
  • Patent number: 5616609
    Abstract: Described are stelleramacrin A and stelleramacrin B represented by the following formulas (I) and (II), respectively: ##STR1## a process for the preparation thereof; and anticancer agents containing either of them as an active ingredient.Therapeutics for solid cancer, said therapeutics containing either of gnidimacrin or pimelea factor P.sub.2 as an active ingredient, are also described.
    Type: Grant
    Filed: February 8, 1994
    Date of Patent: April 1, 1997
    Inventors: Tetsuro Ikekawa, Nobuo Ikekawa
  • Patent number: 5614550
    Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.
    Type: Grant
    Filed: February 27, 1996
    Date of Patent: March 25, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
  • Patent number: 5574173
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.4 is alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha., and methods for treating septic shock, inflammation, or allergic disease.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: November 12, 1996
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Richard J. Friary, Wing C. Tom, Joe F. Lee, Vera A. Seidl
  • Patent number: 5554645
    Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.
    Type: Grant
    Filed: October 3, 1994
    Date of Patent: September 10, 1996
    Assignee: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
  • Patent number: 5539132
    Abstract: Novel compounds for use in inhibiting fatty acid synthesis are disclosed. The compounds can be used for the treatment of tumors or microbial infections.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: July 23, 1996
    Assignees: Johns Hopkins University, Chektec Corporation
    Inventors: Garfield P. Royer, Craig A. Townsend
  • Patent number: 5538986
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: July 23, 1996
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
  • Patent number: 5508444
    Abstract: Novel substituted cis-1,2-dihydroxy-cyclohexadiene compounds, useful as intermediates in the production of compounds for use as intermediates in the production of agrochemicals and pharmaceuticals, and a microbial process for the preparation thereof.
    Type: Grant
    Filed: November 17, 1994
    Date of Patent: April 16, 1996
    Assignee: Zeneca Limited
    Inventors: Andrew J. Blacker, Martin Brown, Martin C. Bowden
  • Patent number: 5436263
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: July 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Sheo B. Singh, Barry A. Katz, Russell B. Lingham, Isabel Martin, Keith C. Silverman
  • Patent number: 5432192
    Abstract: Tricyclic compounds represented by the following formula: ##STR1## wherein X represents --CH.dbd.CH--, --CH.sub.2 O--, or --O--;R.sup.1 represents a lower alkyl group,R.sup.2 represents a hydrogen atom or a lower alkyl group; andn represents an integer of from 1 to 5, pharmacologically acceptable salts thereof, and a method for preparing the same. The present compounds have anti-allergic and anti-histaminic activities and reduced side effects, and are useful as anti-allergic agents and anti-histaminic agents.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: July 11, 1995
    Assignee: Hokuriku Seiyaku Co., Ltd.
    Inventors: Hiroyuki Sawanishi, Yasuo Ito, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kouji Morikawa
  • Patent number: 5430050
    Abstract: The compound of formula, ##STR1## is obtained from cultures of Chaetosphaeronema hispidulum. The compound is an inhibitor of phospholipase C.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: July 4, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tatsuo Ohtsuka, Akiko Sakai, Toru Okuda
  • Patent number: 5412114
    Abstract: The present invention relates to an improvement in the process for preparing a calixarene derivative in which the rotation of its benzene units are hindered and which comprises replacing all or a part of the hydrogen atoms of the hydroxyl groups of a calixarene derivative represented by the general formula: ##STR1## and is characterized by conducting the reaction in the presence of an alkaline earth metal. According to the present invention, an asymmetric calixarene derivative having a "cone" conformation can be selectively prepared by virtue of the template effect of the metal.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: May 2, 1995
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Seiji Shinkai, Tsutomu Matsuda, Takashi Arimura, Hirosuke Kawabata, Kozo Tachibana
  • Patent number: 5360915
    Abstract: A modified alkali metal or ammonium huminate being made from molecules of the group consisting of ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4 are individually hydrogen or --OH, R.sub.2 is ##STR2## or --CH.sub.2 -- and R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, --OH and --OCH.sub.3, with the proviso that R.sub.4, R.sub.5 and R.sub.6 are not all hydrogen at the same time and their preparation and their medical uses.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: November 1, 1994
    Assignee: Rutgerswerke Aktiengesellschaft AG
    Inventors: Urs N. Riede, Bernhard Seubert
  • Patent number: 5340807
    Abstract: 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 --(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: Grant
    Filed: December 11, 1992
    Date of Patent: August 23, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
  • Patent number: 5332857
    Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.
    Type: Grant
    Filed: July 6, 1992
    Date of Patent: July 26, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter A. McCarthy, Frederick J. Walker
  • Patent number: 5302595
    Abstract: Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.
    Type: Grant
    Filed: January 6, 1993
    Date of Patent: April 12, 1994
    Assignee: Pfizer Inc.
    Inventors: Peter E. Cross, Alexander R. MacKenzie
  • Patent number: 5264538
    Abstract: Cyclic poly(aryl ether) oligomers and mixtures thereof, and methods for the preparation thereof in a highly dilute reaction medium under reaction conditions favorable for ring closure at low degrees of polymerization. These oligomers are represented by the general formula ##STR1## where each Y is divalent oxygen or divalent sulfur, each Ar is an aromatic diradical which comprises one or more C.sub.6 to C.sub.20 arylene groups and has at least one electron withdrawing group attached to an aromatic ring, and n is an integer from 1 to about 20 with the proviso that for integer values of n equal to 1 or 2 all linkages between independent aromatic rings comprise at least one atom.
    Type: Grant
    Filed: June 27, 1990
    Date of Patent: November 23, 1993
    Assignee: The Dow Chemical Company
    Inventors: Michael J. Mullins, Edmund P. Woo, Kimberly E. Balon, Daniel J. Murray, Cheng-Cheng C. Chen
  • Patent number: 5242931
    Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: September 7, 1993
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii