Polycyclo Ring System (e.g., Hellebrin, Etc.) Patents (Class 536/18.1)
-
Publication number: 20090074935Abstract: Steviol glycoside isomers are provided having the formula: wherein R1 may be hydrogen, 1-?-D-glucopyranosyl, or 2-(1-?-D-glucopyranosyl)-1-?-D-glucopyranosyl, and R2 may be hydrogen, 1-?-D-glucopyranosyl, 2-(1-?-D-glucopyranosyl)-1-?-D-glucopyranosyl, 2,3-bis(1-?-D-glucopyranosyl)-1-?-D-glucopyranosyl, 2-(1-?-L-rhamnopyranosyl)-1-?-D-glucopyranosyl, 2-(1-?-L-rhamnopyranosyl)-3-(1-?-D-glucopyranosyl)-1-?-D-glucopyranosyl, or 2-(1-?-D-xylopyranosyl)-3-(1-?-D-glucopyranosyl)-1-?-D-glucopyranosyl. Methods for making steviol glycoside isomers are also disclosed. These compounds may be present in food and beverage products as non-nutritive sweeteners.Type: ApplicationFiled: September 17, 2007Publication date: March 19, 2009Applicant: PepsiCo, Inc.Inventor: Thomas Lee
-
Publication number: 20090075919Abstract: The present invention provides a composition for use in treating or preventing neoplasia, comprising an effective actein. The present invention also provides a composition for use in treating or preventing neoplasia, comprising an effective anti-neoplastic amount of an ethyl acetate extract of black cohosh. The present invention further provides a combination of anti-neoplastic agents, comprising an effective anti-neoplastic amount of an ethyl acetate extract of black cohosh and an effective anti-neoplastic amount of at least one additional chemopreventive or chemotherapeutic agent. Methods for treating and preventing neoplasia are also provided.Type: ApplicationFiled: August 4, 2008Publication date: March 19, 2009Inventors: Linda Saxe Einbond, I. Bernard Weinstein
-
Publication number: 20080275226Abstract: The present invention provides the medical use of paeoniflorin in the manufacture of medicaments for treating and preventing apoplexy, Parkinson's diseases and other nervous system diseases.Type: ApplicationFiled: June 27, 2005Publication date: November 6, 2008Inventors: Xingzu Zhu, Dazhi Liu, Yang Ye, Huaqing Liu
-
Patent number: 7429568Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereoType: GrantFiled: October 12, 2005Date of Patent: September 30, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
-
Publication number: 20080221045Abstract: An object of the present invention is to provide a means for improving hepatic function of mammals including humans to normal condition. The present invention achieves the above object by providing a hepatic function-improving agent comprising ?-glucosyl-hesperidin as an effective ingredient.Type: ApplicationFiled: November 21, 2005Publication date: September 11, 2008Applicant: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Hitoshi Mitsuzumi, Mika Takami, Yoshikatsu Miwa, Hiroto Chaen, Toshio Miyake
-
Patent number: 7423133Abstract: Fluorescent glycosides containing aromatic hydrocarbon groups are useful in labelling and detection methods for a wide array of chemical and biological molecules. Assembly of multiple analogs to form “polyfluors” affords fluorescence properties that are different from the properties of the component analogs. This allows for the design and use of combinatorial libraries of molecules displaying widely varying fluorescence colors.Type: GrantFiled: August 22, 2003Date of Patent: September 9, 2008Assignee: The Board of Trustees of the LeLand Stanford Junior UniversityInventors: Eric T. Kool, Jianmin Gao
-
Publication number: 20080199414Abstract: The invention relates to cosmetic formulations, pharmaceutical preparations, food products and food supplements containing flavonoid derivatives. The flavonoid derivatives act therein, for instance, as UV filter. Some flavonoid derivatives represent novel compounds.Type: ApplicationFiled: April 22, 2008Publication date: August 21, 2008Inventors: Corinna Wirth, Herwig Buchholz, Christophe Carola
-
Publication number: 20080188645Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).Type: ApplicationFiled: April 12, 2006Publication date: August 7, 2008Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Graham Ellis-Davies, Atsuya Momotake
-
Publication number: 20080182802Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.Type: ApplicationFiled: December 26, 2007Publication date: July 31, 2008Inventors: Michael J. Hadd, Yuanwei Chen, Yan Feng, Sengen Sen, Brian Seed
-
Patent number: 7393838Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug; one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereType: GrantFiled: October 12, 2005Date of Patent: July 1, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
-
Patent number: 7375087Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents a single bond, a C1-6 alkylene group etc.; Z represents CO or SO2; R4 and R5 represent H, an optionally substituted C1-6 alkyl group etc.; and R3, R6 and R7 represent H, a halogen atom etc.Type: GrantFiled: August 7, 2003Date of Patent: May 20, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hirotaka Teranishi, Nobuhiko Fushimi, Shigeru Yonekubo, Kazuo Shimizu, Toshihide Shibazaki, Masayuki Isaji
-
Patent number: 7375090Abstract: The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on sodium-dependent glucose cotransporter SGLT, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.Type: GrantFiled: August 24, 2004Date of Patent: May 20, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Peter Eickelmann, Leo Thomas, Edward Leon Barsoumian
-
Patent number: 7371730Abstract: The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-?-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.Type: GrantFiled: March 4, 2003Date of Patent: May 13, 2008Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Akira Iyobe, Hirotaka Teranishi, Kazuya Tatani, Shigeru Yonekubo, Masayuki Isaji
-
Patent number: 7371733Abstract: The invention relates to novel paranmycin compounds that have activity against gram positive and gram negative bacteria, preferably bacteria that are resistant to other antibiotics.Type: GrantFiled: March 20, 2006Date of Patent: May 13, 2008Assignee: Utah State UniversityInventor: Cheng-Wei Tom Chang
-
Patent number: 7312200Abstract: The present invention relates to derivatives of 9-keto spinosyns, which are substituted by a ?N—(O, NH or NRx)—Ry moiety in the C-9 position, to methods for their manufacture, and to their use for controlling animal pests.Type: GrantFiled: January 8, 2004Date of Patent: December 25, 2007Assignee: Bayer CropScience AGInventors: Olga Malsam, Peter Lösel, Michael E. Beck, Ulrich Ebbinghaus-Kintscher, Robert Velten, Peter Jeschke, Volker Möhrle, Rita Fröde, Günther Eberz
-
Patent number: 7294618Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1, R2 and R3 represent a hydrogen atom or a halogen atom; R4 represents a lower alkyl group or a halo(lower alkyl) group; and R5 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, etc., a pharmaceutically acceptable salt thereof or a prodrug thereof., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.Type: GrantFiled: February 26, 2002Date of Patent: November 13, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masayuki Isaji
-
Patent number: 7271153Abstract: The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 and X3 independently represent N or CH; X2 represents N or CR2; X4 represents N or CR3; and with the proviso that one or two of X1, X2, X3 and X4 represent N; R1 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group, a lower alkoxy(lower alkoxy)-substituted (lower alkyl) group, a cyclic lower alkyl group, a halo(lower alkyl) group or a group represented by the general formula: HO-A- wherein A represents a lower alkylene group, a lower alkyleneoxy group or a lower alkylenethio group; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic lower alkyl group, a lower alkoxy group, an amino group, a (lower acyl)amino group, a mono(lower alkyl)amino group or a di(lower alkyl)amino group; and R3 represents a hydrogen aType: GrantFiled: June 17, 2002Date of Patent: September 18, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Toshihiro Nishimura, Hideki Fujikura, Nobuhiko Fushimi, Kazuya Tatani, Kenji Katsuno, Masayuki Isaji
-
Patent number: 7262285Abstract: Novel compounds such as compounds designated herein as Xanifolia-Y or -Y3, -Y1, -Y2, -Y8, -Y9 and -Y10 are disclosed. These compounds have anticancer activity. The compounds of the present invention are obtainable from plants in the sapindaceae family, such as Xanthoceras sorbifolia, or other natural sources or products.Type: GrantFiled: May 17, 2005Date of Patent: August 28, 2007Assignee: Pacific Arrow LimitedInventors: Pui-Kwong Chan, May Sung Mak, Yun Wang
-
Patent number: 7217697Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabeticType: GrantFiled: May 27, 2002Date of Patent: May 15, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hiroaki Shiohara, Hideki Fujikura, Nobuhiko Fushimi, Fumiaki Ito, Masayuki Isaji
-
Patent number: 7189702Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.Type: GrantFiled: February 22, 2006Date of Patent: March 13, 2007Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Toshihiro Nishimura, Nobuhiko Fushimi, Hideki Fujikura, Kenji Katsuno, Yoshimitsu Komatsu, Masayuki Isaji
-
Patent number: 7160867Abstract: This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin carbohydrate derivatives having enhanced pharmacokinetic and/or pharmacodynamic profiles. For example, administration of the rapamycin carbohydrate derivative results in altered pharmacokinetic profiles and reduced toxicities. Thus, the present invention provides compounds with characteristics that are distinct from other drugs in its class such as rapamycin.Type: GrantFiled: May 13, 2004Date of Patent: January 9, 2007Assignee: Isotechnika, Inc.Inventors: Mark Abel, Roman Szweda, Daniel Trepanier, Randall W Yatscoff, Robert T. Foster
-
Patent number: 7132403Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.Type: GrantFiled: January 20, 2004Date of Patent: November 7, 2006Assignees: Board of Trustees of Michigan State University, Regents of the University of CaliforniaInventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
-
Patent number: 7105491Abstract: This invention provides nucleic acid sequences and characterization of the gene cluster responsible for the biosynthesis of the enediyne C-1027 (produced by Streptomyces globisporus). Methods are provided for the biosynthesis of enediynes, enediyne analogs and other biological molecules. This invention also provides enediyne and enediyne analogs biosynthesized by manipulation of the C-1027 gene pathway.Type: GrantFiled: November 12, 2002Date of Patent: September 12, 2006Assignee: Wisconsin Alumni Research Foundation (WARF)Inventors: Ben Shen, Wen Liu
-
Patent number: 7101856Abstract: Novel thiophene glycoside derivatives of the formula I: in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for their preparation are disclosed. The compounds are suitable, for example, as antidiabetics.Type: GrantFiled: July 11, 2003Date of Patent: September 5, 2006Assignee: sanofi-aventis Deutschland GmbHInventors: Heiner Glombik, Wendelin Frick, Hubert Heuer, Werner Kramer, Harm Brummerhop, Oliver Plettenburg
-
Patent number: 7087579Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein one of Q and T represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; R1 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkenyl group, a cyclic lower alkyl group, etc.; R2 represents a hydrogen atom, an optionally substituted lower alkyl group, a lower alkoxy group, a lower alkenyl group, a cyclic lower alkyl group, a cyclic lower alkoxy group, etc., which exert an excellent inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutically acceptable salts thereof or prodrugs thereof, production intermediates thereof and pharmaceutical uses thereof.Type: GrantFiled: February 26, 2002Date of Patent: August 8, 2006Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Toshihiro Nishimura, Nobuhiko Fushimi, Hideki Fujikura, Kenji Katsuno, Yoshimitsu Komatsu, Masayuki Isaji
-
Patent number: 7084123Abstract: The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug: one of Q and T represents a group represented by the general formula: (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereoType: GrantFiled: December 25, 2001Date of Patent: August 1, 2006Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi, Toshihiro Nishimura, Takeshi Nakabayashi, Masayuki Isaji
-
Patent number: 7078386Abstract: The present invention relates to a medicament, a food, a beverage or a feed, each comprising as an effective ingredient a compound having an enhancing action for NGF production, which is effective for a treatment, an amelioration of symptom, prevention or the like of a disease requiring enhancement of NGF production, wherein the compound has a coumarin and/or chroman backbone. Since no toxicity is especially found in the effective ingredient of the present invention, and there is no risk of incidence of adverse actions, the treatment or the like of the above disease can be safely and appropriately carried out.Type: GrantFiled: March 28, 2002Date of Patent: July 18, 2006Assignee: Takara Bio, Inc.Inventors: Hiromu Ohnogi, Masahiro Shiraga, Hiroaki Sagawa, Ikunoshin Kato
-
Patent number: 7060686Abstract: Methods for treating, preventing, or inhibiting diseases and disorders associated with inflammation, cell-proliferation, and pain comprising the administration of a compound having the structural formula wherein R1 is a hydrogen, alkyl, aryl, hydroxyalkyl, cycloalkyl, cycloalkenyl, carboxylic acid, alkylamino or amide group having from 2 to 20 carbon atoms, R2, R3, and R4 are each independently hydrogen or an acyl residue having from 1 to 6 carbon atoms, R5 is hydrogen, CH3, or CH2OH, and R6 is an organo group such as a hydrocarbon having from 1 to 10 carbon atoms are disclosed. Other seco-pseudopterosins and compounds related to pseudopterosins are disclosed.Type: GrantFiled: August 2, 2004Date of Patent: June 13, 2006Assignees: The Regents of the University of California, Florida Atlantic University Board of TrusteesInventors: Robert S. Jacobs, Russell G. Kerr
-
Patent number: 7053060Abstract: The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.Type: GrantFiled: November 20, 2001Date of Patent: May 30, 2006Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Nobuhiko Fushimi, Kazuya Tatani, Norihiko Kikuchi, Kenji Katsuno, Masayuki Isaji
-
Patent number: 7052863Abstract: An alizarin-based chromogenic substrate, a composition containing the substrate, and its use to detect the presence of an enzymatic activity are disclosed. The substrate is particularly applicable in the field of biological diagnosis.Type: GrantFiled: December 11, 2000Date of Patent: May 30, 2006Assignee: Biomerieux S. A.Inventors: Lyle Armstrong, Arthur James
-
Patent number: 7049301Abstract: This invention relates to quercetin derivative, its preparation, and a pharmaceutical combination, as well as their medical uses for the prevention or treatment of diseases related to 5HT1A receptor or neuron cell damages, including Alzeheimer's disease, drug or alcohol dependence, sleep disorders or panic state; and for delaying senility, improving learning and memory, preventing and treatment of neuron cell damages caused by various kinds of cerebral damages.Type: GrantFiled: September 26, 2003Date of Patent: May 23, 2006Assignee: Academy of Military Medical Sciences Institute of Pharmacology and ToxicologyInventors: Yimin Zhao, Ming Yang, Yunfeng Li, Xinhui Luan, Zhipu Luo
-
Patent number: 7034130Abstract: The present invention relates to methods for producing novel spinosyn derivatives which are substituted with a 1-hydroxy-ethyl radical in the C-21 position and to novel spinosyn derivatives of this type per se and to their use for producing novel spinosyns.Type: GrantFiled: July 8, 2002Date of Patent: April 25, 2006Assignee: Bayer Cropscience AGInventors: Peter Jeschke, Günther Eberz, Rita Fröde, Volker Möhrle, Robert Velten
-
Patent number: 6927209Abstract: The present invention relates to novel compounds of formula (I): in which: R1, R2 and R3, which are identical or different, are each independently: a (C1-C6)alkyl group, a pyridinyl group or a group —CH2—NR4R5, in which R4 and R5 are each independently a hydrogen atom or a (C1-C4)alkyl group, or alternatively R4 and R5 form, with the nitrogen atom to which they are bonded, a pyrrolidinyl, piperidinyl, hexahydroazepinyl, morpholinyl or piperazinyl group, with the proviso that at least one of the substituents R1, R2 and R3 is other than a (C1-C6)alkyl group, and their salts, solvates and hydrates, especially those which are pharmaceutically acceptable. These compounds are useful particularly for the treatment of disorders of the venous circulation.Type: GrantFiled: May 6, 2002Date of Patent: August 9, 2005Assignee: Laboratoires Fournier S.A.Inventors: Véronique Barberousse, Soth Samreth
-
Patent number: 6887854Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2005Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Hermo N. Jimenez, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugai
-
Patent number: 6875746Abstract: Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof.Type: GrantFiled: January 31, 2003Date of Patent: April 5, 2005Assignee: Board of Trustees of Michigan State UniversityInventors: Muraleedharan G. Nair, Robert H. Cichewicz, Navindra P. Seeram, Yanjun Zhang
-
Patent number: 6872706Abstract: The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein P represents a group forming a prodrug; and R represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a lower alkoxy-substituted (lower alkyl) group, a lower alkoxy-substituted (lower alkoxy) group or a lower alkoxy-substituted (lower alkylthio) group, which have an improved oral absorption and can exert an excellent inhibitory activity in human SGLT2 in vivo and which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutical compositions comprising the same.Type: GrantFiled: September 21, 2001Date of Patent: March 29, 2005Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Nobuhiko Fushimi
-
Patent number: 6867230Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R10 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: June 1, 2001Date of Patent: March 15, 2005Assignee: Pfizer, Inc.Inventors: Matthew Merrill Hayward, Michael S. Visser, Robert G. Linde, II, Takushi Kaneko
-
Patent number: 6849767Abstract: A method of hydroborating an alkene or alkyne, or reducing an organic functionality, oxidizing primary and secondary alcohols using a fluorous borane-sulfide is disclosed. The method includes regeneration and recycling the fluorous borane-sulfide.Type: GrantFiled: July 24, 2003Date of Patent: February 1, 2005Assignee: The Board of Trustees of the University of IllinoisInventors: David C. Crich, Santhosh Neelamkavil
-
Patent number: 6844346Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: December 24, 2002Date of Patent: January 18, 2005Assignees: IBBEX, Inc., Univ. of Alabama at BirminghamInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
-
Publication number: 20040242502Abstract: The present invention discloses novel saponin derivatives for use with nucleic acids that induce an immune response when administered to animals and humans. The novel saponin derivatives disclosed comprise (a) a saponin aglycone core, wherein the aglycone core is covalently linked to one or more oligosaccharide chains; (b) a positively charged cationic chain, and optionally (c) a naturally occurring or synthetic lipophilic chain. Pharmaceutical and veterinary compositions comprising one or more of the novel saponin derivatives and saponin derivative/polynucleotide complexes are also disclosed. Disclosed as well are methods of using the novel saponin derivatives to deliver a polynucleotide molecule to cells of an animal, to stimulate or generate an immune response in an animal, and to generate a detectable immune response in an animal.Type: ApplicationFiled: April 8, 2004Publication date: December 2, 2004Applicant: Galenica Pharmaceuticals, Inc.Inventor: Dante J. Marciani
-
Publication number: 20040242506Abstract: A salt formed from paroxetine hydrochloride and ammonium glycyrrhyzinate masks the bitter taste of paroxetine and has a distinctive liquorice flavour.Type: ApplicationFiled: July 7, 2004Publication date: December 2, 2004Inventors: Nathalie Claude Marianne Barges Causeret, Nicola Lisa Anna Marzolini, Padma Meneaud
-
Publication number: 20040241173Abstract: A fullerene-antibiotic conjugate including at least one antibiotic molecule per fullerene moiety. The fullerene may comprise C60 and the antibiotic may comprise vancomycin or may be selected from the group consisting of penicillins, cephalosporins, quinolones, fluoroquinolones, macrolides, lincosamines, carbepenems, conobactams, aminoglycosides, glycopeptides, tetracyclines, sulfonamides, rifampin, oxazolidonones, and streptogramins. The conjugate preferably includes at least two and more preferably at least three antibiotic molecules per C60 center. A method for making a fullerene(C60)-antibiotic conjugate, comprises: synthesizing a linker precursor (I); reacting the linker precursor (I) with C60 via a Bingel-reaction, to produce a fullerene-linker conjugate (II); hydrolyzing the fullerene-linker conjugate (II), resulting in a desired derivative of C60 (III); and reacting the derivative (III) with a desired antibiotic to produce a fullerene-antibiotic conjugate (IV).Type: ApplicationFiled: February 11, 2004Publication date: December 2, 2004Applicant: William Marsh Rice UniversityInventors: Lon J. Wilson, Andrey L. Mirakyan, Matthew P. Cubbage
-
Patent number: 6818657Abstract: The present invention relates to a ternary glucosyl complex which is a bioprecursor of at least one retinoic active ingredient for percutaneous application, having formula (I), wherein E represents a linear hydrocarbon spacer group that is branched or cyclized and has an aliphatic or aromatic content capable of containing one or several heteroatoms of oxygen and carrying one or several carbonyl groups; A represents a radical of a molecule of said retinoic active ingredient linked to the spacer group by a carboxylate function and n=1 or 2.Type: GrantFiled: September 28, 2001Date of Patent: November 16, 2004Assignee: Pierre Fabre Dermo-CosmetiqueInventors: Daniel Redoules, Roger Tarroux, Didier Fournier, Jean-Jacques Perie
-
Patent number: 6812332Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: January 21, 2003Date of Patent: November 2, 2004Assignees: IBBEX, Inc., UAB Research FoundationInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
-
Patent number: 6800742Abstract: The present invention provides a method for efficiently producing &bgr;-D-ribofuranose derivatives or optical isomers thereof, useful as synthetic intermediates of pharmaceutical nucleic acid-series products. The method comprises a step of producing 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate or an optical isomer thereof by allowing &bgr;-D-ribofuranose-1,2,3,5-tetraacetate or an optical isomer thereof to react with a benzyl alcohol in the presence of acid catalysts and a step of hydrolyzing the resulting 1-O-benzyl-&bgr;-D-ribofuranose-2,3,5-triacetate in the presence of a base to produce 1-O-benzyl-&bgr;-D-ribofuranose or an optical isomer thereof.Type: GrantFiled: March 20, 2002Date of Patent: October 5, 2004Assignee: Ajinomoto Co., Inc.Inventors: Yoshihito Koguchi, Takayoshi Torii, Kunisuke Izawa
-
Publication number: 20040192623Abstract: The invention relates to aloe-emodin (AE) derivatives and their use as anticancer drugs. Saids derivatives show a specific cytotoxicity to tumour cells, also of neuroectodermal origin, to which they may in particular act as aloe-emodin prodrugs. Said pharamcological profile makes them particularly suitable for use in the treatment of neoplasias. Thereofore, pharmaceutical compositions containing said compound may be usefully used in the treatment of neoplasias. It has surprisingly been found that aloe-emodin derivatives in position 3′ (bearing either a positive or negaive charge) exhibit improved sollubility properties and, at the same time, in vitro show cytotoxicity to tumour cells, also of neuroectodermal origin.Type: ApplicationFiled: May 17, 2004Publication date: September 30, 2004Inventors: Giorgio Palu, Modesto Carli, Teresa Pecere, Giuseppe Zagotto
-
Patent number: 6794497Abstract: The present invention provides compounds and methods of synthesizing furanose and aminofuranose compounds of Formula I which are useful fro treating rheumatoid arthritis, immunomodulatory diseases and disorders, inflammation, and diseases and disorders characterized by exhibiting tissue proliferation.Type: GrantFiled: January 22, 2002Date of Patent: September 21, 2004Assignee: Warner-Lambert CompanyInventors: Armen M. Boldi, Elaine B. Krueger, Michael A. Walters, Thutam P. Hopkins, Meghan T. Keaney
-
Patent number: 6784159Abstract: A method of treating polycystic kidney disease is described. The method involves administering soyasaponin Bb to an animal in need thereof.Type: GrantFiled: September 28, 2001Date of Patent: August 31, 2004Assignees: Her Majesty the Queen in right of Canada, as represented by the Minister of Agriculture, University of GuelphInventors: Bruce J. Holub, F. William Collins, Dominique P. Bureau, Diana J. Philbrick
-
Publication number: 20040138151Abstract: Saponins of formula 1Type: ApplicationFiled: January 6, 2004Publication date: July 15, 2004Applicants: Janssen Pharmaceutica N.V., National Center for Science and Technology, Universiteit GentInventors: Louis Jules Roger Marie Maes, Nils Albert Gilbert Germonprez, Luc Emiel Mathilde Van Puyvelde, Norbert G. M. De Kimpe, Tran Ngoc Ninh
-
Patent number: RE38723Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the form XR-SPACER-REPORTER-BLOCK wherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate, -REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate, -SPACER- is a covalent linkage, and XR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R).Type: GrantFiled: August 12, 1997Date of Patent: April 12, 2005Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Ram Sabnis, John Naleway, Nels Olson, Richard P. Haugland