Nitrogen In Aglycone Moiety Patents (Class 536/17.4)
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Publication number: 20030105299Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.Type: ApplicationFiled: October 17, 2001Publication date: June 5, 2003Applicant: MALLINCKRODT INC.Inventors: Samuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj
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Publication number: 20030100742Abstract: The present invention relates to compounds of the formula 1Type: ApplicationFiled: November 20, 2002Publication date: May 29, 2003Applicant: Pfizer Inc.Inventors: Takushi Kaneko, William Thomas McMillen, Yong-Jin Wu
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Patent number: 6566508Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
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Patent number: 6566510Abstract: The invention provides a novel method for synthesizing Morphine-6-Glucuronide comprising the step of reacting 3-O-pivaloyloxymorphine and methyl 1&agr;,2-ethylorthopivalate-3-4,di-O-pivaloylglucouronate.Type: GrantFiled: March 9, 2001Date of Patent: May 20, 2003Assignee: Genes LimitedInventors: Philip James Parsons, Richard Andrew Ewin
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Publication number: 20030092642Abstract: This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-0-methyl-4-C-[(propylamino)methyl]-&agr;-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-&bgr;-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.Type: ApplicationFiled: August 12, 2002Publication date: May 15, 2003Inventors: Robert J. Rafka, Colman B. Ragan, Douglas J. M. Allen
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Publication number: 20030092639Abstract: There are described novel 4′substituted tylosin analogs and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.Type: ApplicationFiled: November 8, 2001Publication date: May 15, 2003Inventors: Ly Tam Phan, Tianying Jian, Yao-Ling Qiu, Yat Sun Or
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Publication number: 20030087843Abstract: A compound of formula I 1Type: ApplicationFiled: September 5, 2002Publication date: May 8, 2003Inventor: William N. Washburn
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Patent number: 6555665Abstract: Glycosidation of 4,5-Epoxymorphinan-6-ols with a Thioglycoside as a glycoside donor is disclosed. The process comprises reacting a 4,5-Epoxymorphinan-6-ol and a Thioglycoside in the presence of a thiophilic promoter under conditions capable of forming 4,5-Epoxymorphinan-6-glycosides. This novel approach was used for preparation of pharmaceutically important 4,5-Epoxymorphinan-6-&bgr;-D-glucuronides. The process provides both high stereo-selectivity and high yields.Type: GrantFiled: September 15, 2000Date of Patent: April 29, 2003Assignee: Cenes LimitedInventors: Arie Gutman, Genadi Nisnevitch, Lev Yudovitch, Igor Rochman
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Publication number: 20030069402Abstract: The invention relates to a process for the production of peracylated 1-O-glycosides of general formula I or salts thereof 1Type: ApplicationFiled: July 11, 2002Publication date: April 10, 2003Applicant: Schering AGInventors: Johannes Platzek, Klaus-Dieter Graske, Ulrich Niedballa
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Patent number: 6545135Abstract: The invention relates to a process for the production of perbenzylated 1-O-glycosides of general formula I or salts thereof in which sugar1 is a monosaccharide that is functionalized in 1-OH-position, R represents benzyl, n means 2, 3 or 4, means —O—, —S—, —COO— or —NH— and L means a straight-chain, branched, saturated or unsaturated C1-C30 carbon chain, which optionally is interrupted or substituted by groups. The process according to the invention starts from economical starting materials, provides good yields and allows the production of perbenzylated saccharides with 1-O-functionalized side chains on an enlarged scale.Type: GrantFiled: March 8, 2001Date of Patent: April 8, 2003Assignee: Schering AktiengesellschaftInventors: Johannes Platzek, Ulrich Niedballa, Peter Mareski
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Publication number: 20030064939Abstract: The invention relates to processes for preparing compounds of formula 1 1Type: ApplicationFiled: April 25, 2002Publication date: April 3, 2003Inventors: Constantine Sklavounos, John L. Tucker, Lulin Wei, Kerry P. Mahon, Philip Hammen, Joanna T. Negri, Richard S. Lehner
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Patent number: 6537971Abstract: This invention provides tissue selective estrogens of formula I having the structure wherein: R1 and R2 are independently, hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, benzoyl, X is hydrogen, alkyl of 1-6 carbon atoms, CN, halogen, trifluoromethyl, or thioalkyl of 1-6 carbon atoms; n=1-3; with the proviso that at least one of R1 or R2 are not hydrogen, alkyl chain of 1-6 carbon atoms, benzyl, acyl of 2-7 carbon atoms, or benzoyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 1, 2002Date of Patent: March 25, 2003Assignee: WyethInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Anita Wai-Yin Chan, Arkadiy Z. Rubezhov
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Publication number: 20030050256Abstract: Sugar-modified SIN-1 compositions are provided. The compositions are useful for generating NO in response to hydrolytic activity of a glycosidase specific for the O-glycosidic bond between the sugar and SIN-1 moieties. Pharmaceutical compositions containing the sugar-modified SIN-1 compositions and methods of using the compositions are also provided.Type: ApplicationFiled: August 9, 2001Publication date: March 13, 2003Inventors: Peng George Wang, Xuejun Wu, Xiaoping Tang
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Publication number: 20030050257Abstract: Glucoside and glucuronide derivatives of hydromorphone, dihydromorphine, and dihydroisomorphine and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising a glucoside or glucuronide derivative of hydromorphone, dihydromorphine, or dihydroisomorphine or a pharmaceutically acceptable salt thereof, and methods for treating or preventing pain in a patient comprising administering to a patient in need thereof a glucoside or glucuronide derivative of hydromorphone, dihydromorphine, or dihydroisomorphine or a pharmaceutically acceptable salt thereof are disclosed.Type: ApplicationFiled: July 22, 2002Publication date: March 13, 2003Inventors: Feng Gao, Jahanara Miotto
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Patent number: 6531449Abstract: The invention provides metabolites of the compound 2-amino-N-[2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-[4,3-c]pyridin-5-yl)-1-(R)-benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide, the racemic-diastereomeric mixtures and optical isomers thereof, the prodrugs thereof, and the pharmaceutically acceptable salts of the metabolites, racemic-diastereomeric mixtures, optical isomers, and prodrugs; to pharmaceutical compositions thereof; and to methods of using the metabolites and the compositions in the treatment of diseases associated with reduced levels of growth hormone.Type: GrantFiled: March 8, 2001Date of Patent: March 11, 2003Assignee: Pfizer Inc.Inventors: S. Cyrus Khojasteh, John P. O'Donnell
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Publication number: 20030036538Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.Type: ApplicationFiled: July 3, 2001Publication date: February 20, 2003Applicant: MALLINCKRODT INC.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Publication number: 20030031676Abstract: Disclosed are compounds which are conjugates of (a) a moiety capable of localizing in the cells of a tumor or atheroma and (b) a moiety capable of catalyzing the production of reactive oxygen species from a cellular metabolite. The disclosed compounds which are useful for treating atheroma, tumors and other neoplastic tissue.Type: ApplicationFiled: May 30, 2002Publication date: February 13, 2003Applicant: Pharmacyclics, Inc.Inventors: Jonathan L. Sessler, Darren Magda
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Patent number: 6515117Abstract: An SGLT2 inhibiting compound is provided having the formula A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.Type: GrantFiled: May 20, 2002Date of Patent: February 4, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Bruce Ellsworth, William N. Washburn, Philip M. Sher, Gang Wu, Wei Meng
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Publication number: 20030023081Abstract: High purity pharmaceutical-grade water-soluble porphyrin derivatives having a general formula given by formula 1 or 2 and new methods to prepare and use such porphyrin derivatives: 1Type: ApplicationFiled: May 20, 2002Publication date: January 30, 2003Applicant: CeramOptec Industries Inc.Inventors: Nikolay E. Nifantiev, Dmitri V. Yashunsky
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Patent number: 6512100Abstract: 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: August 30, 2000Date of Patent: January 28, 2003Assignees: Ibbex, Inc., UAB Research FoundationInventors: Stephen C Johnson, Ashraf Saeed, Ming Luo
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Patent number: 6512101Abstract: Branched hydrazone linkers for linking a targeting ligand such as an antibody to a therapeutically active drug. The point of branching is at a polyvalent atom and the number of drugs increases by a factor of two for each generation of branching. A preferred drug is doxorubicin.Type: GrantFiled: August 19, 1998Date of Patent: January 28, 2003Assignee: Bristol Myers Squibb CompanyInventors: Dalton King, Raymond A. Firestone, Pamela Trail
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Publication number: 20030017164Abstract: The present invention discloses dye-azide derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and nitrene at the lesion of interest.Type: ApplicationFiled: July 3, 2001Publication date: January 23, 2003Applicant: MALLINCKRODT INC.Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard B. Dorshow
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Publication number: 20030013861Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): 1Type: ApplicationFiled: July 24, 2002Publication date: January 16, 2003Inventors: Long Y. Chiang, Vijayaraj Anantharaj
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Publication number: 20030013860Abstract: Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.Type: ApplicationFiled: January 24, 2001Publication date: January 16, 2003Inventor: Wayne A. Boettner
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Publication number: 20030013663Abstract: 6-O-Carbamoyl ketolide antibacterials of the formula: 1Type: ApplicationFiled: February 1, 2001Publication date: January 16, 2003Inventors: Todd C. Henninger, Xiaodong Xu
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Patent number: 6506734Abstract: The present invention relates to glycoconjugates of 20(S)-camptothecin, in which a 3-O-methylated &bgr;-L-fucose unit is linked to the 20-hydroxyl group of a camptothecin derivative via a thiourea-modified peptide spacer. The invention furthermore relates to processes for the preparation of the compounds according to the invention and to their use as medicaments, in particular in connection with oncoses.Type: GrantFiled: October 27, 1999Date of Patent: January 14, 2003Assignee: Bayer AktiengesellschaftInventors: Hans-Georg Lerchen, Karsten von dem Bruch, Jörg Baumgarten, Michael Sperzel
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Publication number: 20030004334Abstract: The invention relates to the chemistry of biologically active compounds, namely, to a new method to prepare water-soluble porphyrin derivatives, particularly chlorin derivatives having general formulae (1). The compounds of the present invention are useful as photosensitizers for the photodynamic therapy of cancer, of infectious and other diseases, as well as for light irradiation treatments in other cases.Type: ApplicationFiled: June 1, 2001Publication date: January 2, 2003Applicant: CeramOptec Industries, Inc.Inventor: Nikolay E. Nifantiev
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Publication number: 20020198157Abstract: Purpurin-carbohydrate conjugates and their method of preparation and use for treatment of cancer cells.Type: ApplicationFiled: May 7, 2002Publication date: December 26, 2002Inventors: Ravindra K. Pandey, Thomas J. Dougherty
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Publication number: 20020187941Abstract: In accordance with the present invention, there is provided pregabalin lactose conjugate compounds.Type: ApplicationFiled: January 28, 2002Publication date: December 12, 2002Inventors: Timothy Robert Hurley, Michael James Lovdahl, Brian Tobias
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Publication number: 20020183267Abstract: The present invention relates to a compound named Vancoresmycin which is obtainable by cultivation of the microorganism HIL-006734 (DSM 12216), and to its pharmaceutically acceptable salts. The present invention further relates to a process for the production of Vancoresmycin, to the microorganism HIL-006734 (DSM 12216), to the use of Vancoresmycin and its pharmaceutically acceptable salts as pharmaceuticals, and in particular to their use as antibiotics, and to pharmaceutical compositions comprising Vancoresmycin or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 25, 2002Publication date: December 5, 2002Inventors: Nirogi Venkata Satya Ramakrishna, Ravi Gaianan Bhat, Eyyammadichiyil Sankaranarayanan Sreekumar, Erra Koteswara Satya Vijayakumar, Shantilal Dayaram Naker, Uttara Vinayak Oak, Rajendra Prakash Tanpure, Cordula Hopmann, Michael Kurz, Joachim Wink, Gerhard Seibert, Dominique Le Beller, Jozsef Aszodi
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Patent number: 6486129Abstract: The present invention relates to compounds of formula (1), wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substitutents selected from (1-8C)alkyl or (1-8C)alkoxy; R2 and R3 are independently H or (1-8C)alkyl; R4 is (1-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(1-8C)alkyl; Q is a spacer having a chain length of 10 to 70 atoms; and Z is a negatively charged oligosaccharide residue comprising two to six monosaccharide units, the charge being compensated by positively charged counterions; or a pharmaceutically acceptable salt thereof or a prodrug thereof.Type: GrantFiled: December 18, 2000Date of Patent: November 26, 2002Assignees: Akzo Nobel N.V., University LeidenInventors: Cornelia Maria Tromp, Johannes Egbertus Maria Basten, Constant Adriaan Anton van Boeckel, Rogier Christian Buijsman
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Patent number: 6479650Abstract: The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an &agr; or &bgr; configuration. The subject compounds are useful as probes in the study of the structure and dynamics of nucleic acids and their complexes with proteins. In addition, the subject compounds are useful in any technique which uses labeled oligonucleotides for detection. Non-fluorescent spacer molecules in which a cyclohexane, cyclohexene, decalin, or benzene is joined to a carbon of a sugar moiety such as pentose, hexose, ribose or deoxyribose are also provided. Also provided are the 5′ dimethoxytrityl-3′-O-phosphoramidite derivatives, suitable for incorporation into oligonucleotides by automated synthesizers.Type: GrantFiled: December 14, 1999Date of Patent: November 12, 2002Assignee: Research Corporation Technologies, Inc.Inventor: Eric T. Kool
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Publication number: 20020160966Abstract: Bicyclic leucomycins and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compoundsType: ApplicationFiled: February 16, 2001Publication date: October 31, 2002Inventors: Yat Sun Or, Sophie Binet, Ly Tam Phan
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Publication number: 20020156026Abstract: This invention relates to compounds of formula (1) and to pharmaceutically acceptable salts thereof. The compounds of formula (1) are potent antibacterial agents that may be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula (1) and to methods of treating bacterial infections by administering the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1) and to intermediates useful in such preparation.Type: ApplicationFiled: February 26, 2002Publication date: October 24, 2002Inventors: Brain Scott Bronk, Takushi Kaneko, Michael Anthony Letavic, Hengmaio Cheng, Edward Alan Glazer, Bingwei Vera Yang
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Publication number: 20020156027Abstract: This invention relates to compounds of the formula 1 1Type: ApplicationFiled: April 5, 2002Publication date: October 24, 2002Inventors: William T. McMillen, Takushi Kaneko
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Publication number: 20020155999Abstract: An anti-cancer substance has a porphyrin-like molecule conjugated to an anti-cancer drug. In one embodiment, the porphyrin-like molecule is conjugated directly to an anti-cancer drug. In a second embodiment, the porphyrin-like molecule is conjugated to a first end of a peptide chain, while a second end of the peptide chain is conjugated to the anti-cancer drug. The peptide chain is designed to be cleaved under physiological conditions surrounding the tumor. In the preferred embodiment, the peptide chain functions as a protease inhibitor once it has been cleaved.Type: ApplicationFiled: March 22, 2002Publication date: October 24, 2002Inventor: In Suk Han
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Publication number: 20020151507Abstract: The invention relates to compounds of formula (I), and to pharmaceutically acceptable salts thereof, wherein R1, R2, R6 and X are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula (I), methods of using said compounds of formula (I) in the treatment of bacterial and protozoa infections, and methods of preparing said compounds of formula (I).Type: ApplicationFiled: March 26, 2002Publication date: October 17, 2002Inventor: Yong-Jin Wu
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Publication number: 20020142971Abstract: This invention provides tissue selective estrogens of formula I having the structure 1Type: ApplicationFiled: March 1, 2002Publication date: October 3, 2002Applicant: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Anita Wai-Yin Chan, Arkadiy Z. Rubezhov
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Publication number: 20020137689Abstract: Compounds of the formula I, 1Type: ApplicationFiled: December 19, 2001Publication date: September 26, 2002Inventors: Heiner Glombik, Werner Krame, Stefanie Flohr, Wendelin Frick, Hubert Heuer, Gerhard Jaehne, Andreas Lindenschmidt, Hans-Ludwig Schafer
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Publication number: 20020137690Abstract: please check closely-very confusing Hypocholesterolemic sugar-substituted 2-azetidinone compounds of the formula: 1Type: ApplicationFiled: December 17, 2001Publication date: September 26, 2002Applicant: Schering CorporationInventors: Anima Ghosal, Shmuel Zbaida, Swapan K. Chowdhury, Robert M. Iannucci, Wenqing Feng, Kevin B. Alton, James E. Patrick, Harry R. Davis
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Publication number: 20020115620Abstract: 6-O-Carbamoyl ketolide antibacterials of the formula: 1Type: ApplicationFiled: December 5, 2001Publication date: August 22, 2002Inventors: Todd C. Henninger, Xiaodong Xu
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Publication number: 20020111318Abstract: An improved process for preparing non-hygroscopic Azithromycin dihydrate wherein Azithromycin monhydrate can be converted to Azithromycin dihydrate with continous stirring/agitation in presence of a mixture of at least one solvent and water until non-hygroscopic crystals of Azithromycin dihydrate are obtained. The solvent used in the process can be selected from the group comprising dimethylformamide, dimethylacetamide, acetonitrile and iso-propanol.Type: ApplicationFiled: January 18, 2002Publication date: August 15, 2002Inventor: Srinivasan Rengaraju
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Publication number: 20020107207Abstract: The present invention provides an antiproliferative compound having a structural formula 1Type: ApplicationFiled: November 5, 2001Publication date: August 8, 2002Inventors: Bob G. Sanders, Kimberly Kline, Weiping Yu
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Publication number: 20020103140Abstract: The present invention relates to 6-O-alkyl-2-nor-2-substituted ketolide compound or a derivative thereof, a composition comprising the compound and a suitable carrier, a method of preparing the compound, and a method of treatment and prevention of in mammals comprising administering said compound.Type: ApplicationFiled: November 30, 2000Publication date: August 1, 2002Inventors: Ly Tam Phan, Yat Sun Or, Zhenkun Ma
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Publication number: 20020095026Abstract: Coumermycin analogs of general formula I: 1Type: ApplicationFiled: April 23, 2001Publication date: July 18, 2002Inventors: Michael A. Farrar, Steven H. Olson, Roger M. Perlmutter, Llnon H. Slossberg
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Publication number: 20020095029Abstract: This invention relates to a metal complex of formula (I). The metal complex is capable of cleaving a bulge-containing nucleic acid at the bulge site with high specificity.Type: ApplicationFiled: January 2, 2002Publication date: July 18, 2002Applicant: Academia Sinica, a Taiwan corporationInventors: Chien-Chung Cheng, Wen Jwu Wang
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Publication number: 20020094962Abstract: The present invention provides novel macrolide compounds of the formulas 1Type: ApplicationFiled: November 21, 2001Publication date: July 18, 2002Inventors: Gary Ashley, Brian Metcalf, Zong-Qiang Tian, Daniel Santi
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Patent number: 6414126Abstract: SGLT2 inhibiting compounds are provided having the formula where R1, R2, and R2a are independently hydrogen, OH, OR5, lower alkyl, CF3, OCHF2, OCF3, SR5i or halogen, or two of R1, R2 and R2a together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R3 and R4 are independently hydrogen, OH, OR5a, OAryl, OCH2Aryl, lower alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CN, —CO2R5b, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5h)R6d, —CONR6R6a, —NHCOR5c, —NHSO2R5d, —NHSO2Aryl, Aryl, —SR5e, —SOR5f, —SO2R5g, —SO2Aryl, or a five, six or seven membered heterocycle, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently lower alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl,Type: GrantFiled: October 4, 2000Date of Patent: July 2, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Bruce Ellsworth, William N. Washburn, Philip M. Sher, Gang Wu, Wei Meng
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Publication number: 20020082399Abstract: It is possible to prepare cationic derivatives of fructans, such as inulin, in which a nitrogen atom having substituents R1, R2 and R3 is bonded to one or more anhydrofructose units via a straight-chain or branched C2-C6 alkylene group, which is optionally preceded by a carbonyl group or interrupted by one or two oxygen atoms or imino or alkylimino groups and optionally substituted by one or two hydroxyl groups or amine groups or a carboxyl or carbamoyl group, the substituents R1, R2 and R3 having the following meaning: R1 and R2 each represent hydrogen, methyl carboxymethyl, phosphonomethyl, ethyl, hydroxyethyl, propyl, isopropyl, allyl, hydroxypropyl or dihydroxypropyl or, together with the nitrogen atom, form a cyclic group, R3 represents hydrogen, C1-C18 alkyl, C3-C18 alkenyl, alkynyl or cycloalkyl, C4-C18 cycloalkyl-alkyl or C7-C18 aralkyl or is bondedvia an alkylene group to an oxygen atom of a subsequent anhydrofructose unit.Type: ApplicationFiled: March 18, 1999Publication date: June 27, 2002Inventors: HENDRIKA CORNELIA KUZEE, MARIETTE ELLEN BOUKJE BOLKENBAAS, RONALD JONKER
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Publication number: 20020076379Abstract: Perfluoroalkyl-containing complexes with sugar radicals of general formula I 1Type: ApplicationFiled: August 10, 2001Publication date: June 20, 2002Applicant: Schering AGInventors: Johannes Platzek, Peter Mareski, Ulrich Niedballa, Bernd Raduechel, Hanns-Joachim Weinmann, Bernd Misselwitz