Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/354)
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Patent number: 6312738Abstract: 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: GrantFiled: January 14, 2000Date of Patent: November 6, 2001Assignee: Neem Extracts Pty. Ltd.Inventors: Michael J. O'Shea, Donald J. Brushett, David J. Pollard
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Patent number: 6307068Abstract: 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: GrantFiled: December 14, 2000Date of Patent: October 23, 2001Assignee: Adir et CompagnieInventors: Ying Li, Feng Shan, Jin Ming Wu, Guangshao Wu, Jian Ding, Jianxian Han, Ghanem Atassi, Pierre Renard
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: 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: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: 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: 6271425Abstract: 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: GrantFiled: September 7, 1999Date of Patent: August 7, 2001Assignees: Fujisawa Pharmaceutical Co., Ltd.Inventors: Eiichi Nakamura, Masaya Sawamura
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Patent number: 6245806Abstract: 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: GrantFiled: July 25, 2000Date of Patent: June 12, 2001Assignee: Merck & Co., Inc.Inventors: Anne Dombrowski, Sheo Singh, Deborah L. Zink, Ana Teran, Fernando Pelaez, Daria Hazuda
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Patent number: 6225338Abstract: 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: GrantFiled: October 15, 1998Date of Patent: May 1, 2001Assignee: Mars IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Patent number: 6187543Abstract: 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: GrantFiled: April 19, 1999Date of Patent: February 13, 2001Assignee: Duke UniversityInventor: Perry J. Blackshear
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Patent number: 6156282Abstract: 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: GrantFiled: January 27, 1999Date of Patent: December 5, 2000Assignee: Commissariat a l'Energie AtomiqueInventors: Jean-Fran.cedilla.ois Dozol, Veronique Lamare, Christophe Bressot, Rocco Ungaro, Alessandro Casnati, Jacques Vicens, Zouhair Asfari
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Patent number: 6100293Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 1, 1998Date of Patent: August 8, 2000Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Shouwu Miao, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 6060468Abstract: 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: GrantFiled: October 3, 1997Date of Patent: May 9, 2000Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Erik Fischer, Rolf Hohlweg, Knud Erik Andersen, Uffe Bang Olsen, Zdenek Polivka, Vladimir Valenta, Karel Sindelar
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Patent number: 6057441Abstract: 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: GrantFiled: October 6, 1998Date of Patent: May 2, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Pilar Gil-Lopetegui, Francisco Javier Fernandez-Gadea, Theo Frans Meert
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Patent number: 6054448Abstract: 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: GrantFiled: October 17, 1997Date of Patent: April 25, 2000Assignee: Eli Lilly and Company LimitedInventors: Barry Peter Clark, John Richard Harris
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Patent number: 5990104Abstract: 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: GrantFiled: March 25, 1998Date of Patent: November 23, 1999Assignee: Biochem Pharma, Inc.Inventors: John Dimaio, Dilip M. Dixit
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Patent number: 5948817Abstract: 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: GrantFiled: March 4, 1998Date of Patent: September 7, 1999Assignee: Bristol-Myers Squibb CompanyInventors: James Epperson, Graham Johnson, Daniel J. Keavy, Katherine S. Takaki
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Patent number: 5926687Abstract: 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: GrantFiled: October 4, 1995Date of Patent: July 20, 1999Assignee: Commissariat a l'Energie AtomiqueInventors: Jean-Fran.cedilla.ois Dozol, Helene Rouquette, Rocco Ungaro, Alessandro Casnati
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Patent number: 5917057Abstract: 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: GrantFiled: February 27, 1998Date of Patent: June 29, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
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Patent number: 5883119Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 16, 1996Date of Patent: March 16, 1999Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5843986Abstract: 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: GrantFiled: October 19, 1995Date of Patent: December 1, 1998Assignee: Adir et CompagnieInventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Hamid Ait Mansour, Philippe Delagrance, Pierre Renard
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Patent number: 5840749Abstract: 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: GrantFiled: March 8, 1994Date of Patent: November 24, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Richard C. Allen, Grover C. Helsley, R. Richard L. Hamer, Brian S. Freed, John I. White, Lawrence L. Martin
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Patent number: 5789496Abstract: 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: GrantFiled: January 24, 1997Date of Patent: August 4, 1998Assignee: IBC Advanced Technologies, Inc.Inventors: Bryon J. Tarbet, Garren Maas, Krzysztof E. Krakowiak, Ronald L. Bruening
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Patent number: 5780500Abstract: 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: GrantFiled: April 18, 1997Date of Patent: July 14, 1998Assignee: Novartis CorporationInventors: Claudia Betschart, Kaspar Zimmermann
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Patent number: 5780501Abstract: 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: GrantFiled: July 8, 1997Date of Patent: July 14, 1998Assignee: Novartis CorporationInventors: Claudia Betschart, Kaspar Zimmermann
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Patent number: 5773262Abstract: 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: GrantFiled: February 6, 1997Date of Patent: June 30, 1998Assignee: Kikkoman CorporationInventors: Toshiaki Ariga, Hiroshi Hosoyama, Katsumi Yuasa
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Patent number: 5741814Abstract: 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: GrantFiled: September 3, 1996Date of Patent: April 21, 1998Assignee: Nissan Chemical Industries, Ltd.Inventors: Yasuyuki Nakajima, Hisayuki Watanabe, Michiaki Adachi, Michito Tagawa, Mitsugu Futagawa, Takashi Furusato, Hiroshi Ohya, Masanori Nishioka
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Patent number: 5728727Abstract: 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: GrantFiled: October 3, 1996Date of Patent: March 17, 1998Assignee: American Home Products CorporationInventors: Michael H. Su, Margaret I. Hosken, Brian J. Hotovec, Terra L. Johnston
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Patent number: 5726325Abstract: 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: GrantFiled: June 6, 1997Date of Patent: March 10, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Makoto Yoshida, Shin-ichi Sasaki, Shigeru Aono, Shigeki Fujiwara, Haruki Takai, Tsuyoshi Yamagata, Ken Nagashima, Akira Karasawa
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Patent number: 5726203Abstract: 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: GrantFiled: May 21, 1996Date of Patent: March 10, 1998Inventors: Zelin Li, Xuande Luo, Yi Zeng, Lin Ma
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Patent number: 5712305Abstract: 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: GrantFiled: July 26, 1996Date of Patent: January 27, 1998Assignee: MARS, IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Patent number: 5695763Abstract: 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: GrantFiled: February 14, 1996Date of Patent: December 9, 1997Assignee: Trifolio-M GmbH, Herstellung Und VertriebInventor: Hubertus Kleeberg
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Patent number: 5696156Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 16, 1996Date of Patent: December 9, 1997Assignee: Merck & Co. Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5679703Abstract: 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: GrantFiled: September 7, 1995Date of Patent: October 21, 1997Assignee: Kyowa Hakko Kogyo, Co., Ltd.Inventors: Masashi Yanase, Toshiaki Kumazawa, Shiro Shirakura, Eiko Oishi, Koji Yamada
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Patent number: 5679705Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 16, 1996Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 5656702Abstract: 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: GrantFiled: November 4, 1994Date of Patent: August 12, 1997Assignee: IBC Advanced Technologies, Inc.Inventors: Bryon J. Tarbet, Garren Maas, Krzysztof E. Krakowiak, Ronald L. Bruening
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Patent number: 5616609Abstract: 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: GrantFiled: February 8, 1994Date of Patent: April 1, 1997Inventors: Tetsuro Ikekawa, Nobuo Ikekawa
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Patent number: 5614550Abstract: 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: GrantFiled: February 27, 1996Date of Patent: March 25, 1997Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Koza Oda, Sadao Ishihara, Fujio Saito, Hiroyuki Koike, Teiichiro Koga, Eiichi Kitazawa, Hiroshi Kogen, Ichiro Hayakawa
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Patent number: 5574173Abstract: 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: GrantFiled: December 6, 1993Date of Patent: November 12, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Richard J. Friary, Wing C. Tom, Joe F. Lee, Vera A. Seidl
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Patent number: 5554645Abstract: 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: GrantFiled: October 3, 1994Date of Patent: September 10, 1996Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Patent number: 5539132Abstract: 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: GrantFiled: January 24, 1994Date of Patent: July 23, 1996Assignees: Johns Hopkins University, Chektec CorporationInventors: Garfield P. Royer, Craig A. Townsend
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Patent number: 5538986Abstract: 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: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5508444Abstract: 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: GrantFiled: November 17, 1994Date of Patent: April 16, 1996Assignee: Zeneca LimitedInventors: Andrew J. Blacker, Martin Brown, Martin C. Bowden
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Patent number: 5436263Abstract: 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: GrantFiled: March 22, 1994Date of Patent: July 25, 1995Assignee: Merck & Co., Inc.Inventors: Sheo B. Singh, Barry A. Katz, Russell B. Lingham, Isabel Martin, Keith C. Silverman
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Patent number: 5432192Abstract: 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: GrantFiled: October 1, 1993Date of Patent: July 11, 1995Assignee: Hokuriku Seiyaku Co., Ltd.Inventors: Hiroyuki Sawanishi, Yasuo Ito, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kouji Morikawa
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Patent number: 5430050Abstract: The compound of formula, ##STR1## is obtained from cultures of Chaetosphaeronema hispidulum. The compound is an inhibitor of phospholipase C.Type: GrantFiled: November 22, 1993Date of Patent: July 4, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Tatsuo Ohtsuka, Akiko Sakai, Toru Okuda
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Patent number: 5412114Abstract: 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: GrantFiled: February 9, 1993Date of Patent: May 2, 1995Assignee: Daicel Chemical Industries, Ltd.Inventors: Seiji Shinkai, Tsutomu Matsuda, Takashi Arimura, Hirosuke Kawabata, Kozo Tachibana
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Patent number: 5360915Abstract: 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: GrantFiled: October 14, 1992Date of Patent: November 1, 1994Assignee: Rutgerswerke Aktiengesellschaft AGInventors: Urs N. Riede, Bernhard Seubert
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Patent number: 5340807Abstract: 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: GrantFiled: December 11, 1992Date of Patent: August 23, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5332857Abstract: 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: GrantFiled: July 6, 1992Date of Patent: July 26, 1994Assignee: Pfizer Inc.Inventors: Peter A. McCarthy, Frederick J. Walker
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Patent number: 5302595Abstract: 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: GrantFiled: January 6, 1993Date of Patent: April 12, 1994Assignee: Pfizer Inc.Inventors: Peter E. Cross, Alexander R. MacKenzie
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Patent number: 5264538Abstract: 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: GrantFiled: June 27, 1990Date of Patent: November 23, 1993Assignee: The Dow Chemical CompanyInventors: Michael J. Mullins, Edmund P. Woo, Kimberly E. Balon, Daniel J. Murray, Cheng-Cheng C. Chen
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Patent number: 5242931Abstract: 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: GrantFiled: March 23, 1992Date of Patent: September 7, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii