Nitrogen Containing Hetero Ring Patents (Class 536/17.3)
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Patent number: 11773127Abstract: The present invention is directed to various compounds, compositions, and methods for treating bacterial infections such as urinary tract infections.Type: GrantFiled: November 8, 2018Date of Patent: October 3, 2023Assignee: Washington UniversityInventors: Vasilios Kalas, James W. Janetka, Scott Hultgren, Jerry Pinkner, Amarendar Maddirala, Vishnu Damalanka
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Patent number: 8952140Abstract: A compound having a structure expressed by the following General Formula (1) or a salt thereof where “R” denotes a hydrogen atom or an alkyl group.Type: GrantFiled: February 23, 2012Date of Patent: February 10, 2015Assignee: Microbial Chemistry Research FoundationInventor: Shigehiro Tohyama
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Patent number: 8716472Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.Type: GrantFiled: October 16, 2007Date of Patent: May 6, 2014Assignee: University of RochesterInventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
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Publication number: 20130225514Abstract: The present invention relates to a C-aryl glucoside derivative of Formula (I) below, a preparation method therefor and a use thereof, wherein X, R1, R2, R3, R4, m and n are as defined in specification. The derivative of the present invention is a sodium-glucose co-transporter 2 (SGLT-2) inhibitor associated with glucose reabsorption of bowel or kidney, and has a good urine glucose excreting effect, thus being useful as a therapeutic agent for treating diabetes and related diseases.Type: ApplicationFiled: October 27, 2011Publication date: August 29, 2013Applicant: SHANGHAI ALLIST PHARMACEUTICALS, INC.Inventor: Huibing Luo
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Patent number: 8507660Abstract: A novel N-acetyl-5-N,4-O-carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and ?-selectivity is disclosed. Methods for making disaccharide building blocks comprising ?(2?3), ?(2?6), ?(2?8), ?(2?8)/?(2?9) alternate, and ?(2?9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutinin (HA) from various strains of influenza are provided.Type: GrantFiled: March 29, 2010Date of Patent: August 13, 2013Assignee: Academia SinicaInventors: Chi-Huey Wong, Ting-Jen Rachel Cheng, Chung-Yi Wu
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Patent number: 8507661Abstract: The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose. The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.Type: GrantFiled: February 26, 2010Date of Patent: August 13, 2013Assignee: Alnylam Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Venkitasamy Kesavan, Kallanthottathil G. Rajeev
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Publication number: 20130203975Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: April 12, 2012Publication date: August 8, 2013Applicant: NOVARTIS AGInventors: Gregory Raymond Bebernitz, Mark Gary Bock
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Patent number: 8461122Abstract: The disclosure relates to derivatives of morphine-6-glucuronide of formula (I) wherein R1 is as defined in the disclosure, or an acid addition salt thereof, as well as in hydrate or solvate form. The disclosure also relates to the preparation method thereof and to the use of same in therapeutics.Type: GrantFiled: June 8, 2011Date of Patent: June 11, 2013Assignee: SanofiInventors: Alain Dlubala, Claire Trecant, Isabelle Ripoche
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Patent number: 8445450Abstract: The present invention relates compounds of the formula (I) oligosaccharide-spacer-A??(I), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO2—R1][CO—NR2—CH(4-benzamidine)-CO—NR3R4].Type: GrantFiled: April 4, 2012Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme B.V.Inventors: Martin De Kort, Constant Adriaan Anton Van Boeckel
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Patent number: 8440634Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.Type: GrantFiled: June 8, 2011Date of Patent: May 14, 2013Assignee: SanofiInventors: Alain Dlubala, Claire Trecant, Isabelle Ripoche
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Patent number: 8354382Abstract: The present invention provides a novel form of 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.Type: GrantFiled: April 13, 2009Date of Patent: January 15, 2013Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Takeuchi, Eiji Tsuru
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Publication number: 20120214754Abstract: The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R1 is an O-alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R2 is an OSO3? or hydroxyl group, R3 is an alkyl, cycloalkyl, or alkyl-cycloalkyl group, R4 is a disaccharide having Formula (II), R6 is a disaccharide having Formula (III), and R8 is a disaccharide having Formula (IV), where R5, R7, and R9 are OSO3? or hydroxyl groups. The invention further relates to the preparation of said octasaccharides and to the therapeutic use thereof.Type: ApplicationFiled: February 9, 2012Publication date: August 23, 2012Applicant: SANOFIInventors: Pierre Alexandre DRIGUEZ, Philippe DUCHAUSSOY, Pierre FONS, Corentin HERBERT, Gilbert LASSALLE
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Publication number: 20120190543Abstract: The present invention concerns novel heteroaryl-N-aryl carbamates and their use in pest control, as insecticides and acaricides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: William T. Lambert, Gary D. Crouse, Thomas C. Sparks, Denise P. Cudworth
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Publication number: 20120172321Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 1, 2012Publication date: July 5, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Young K. Chen, Erick Co, Prasuna Guntupalli, John D. Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
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Patent number: 8173608Abstract: The present invention relates to a compound represented by the following formula (1?) wherein R is an aldopyranose residue, R2 is a C2-18 hydrocarbon group optionally having substituent(s), R3 is an acyl group, X is an oxygen atom, a sulfur atom or —NH—, and p is an integer of 0-4, or a salt thereof. The compound of the present invention has a specific immunoregulatory ability, and is useful for the prophylaxis or treatment of autoimmune diseases and the like.Type: GrantFiled: March 3, 2006Date of Patent: May 8, 2012Assignee: RikenInventors: Ken-ichi Fuhshuku, Kenji Mori, Takuya Tashiro, Masaru Taniguchi, Ken-ichiro Seino
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Publication number: 20120108529Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
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Patent number: 8168595Abstract: The present invention relates to compounds of the formula (I) oligosaccharide-spacer-A (1), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO2—R1[CO—NR2—CH(4-benzamidine)-CO—NR3R4], 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 substituents selected from (1-8C)alkyl or (1-8C)alkoxy; and wherein R2 and R3 are independently H or (1-8C)alkyl; R4 is (-8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atomType: GrantFiled: December 21, 2005Date of Patent: May 1, 2012Assignee: Msd Oss B.VInventors: Martin De Kort, Constant Adriaan Anton Van Boeckel
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Publication number: 20120095197Abstract: Methods of synthesizing sodium glucose co-transporter 2 inhibitors, as well as compounds useful therein, are disclosed.Type: ApplicationFiled: August 11, 2011Publication date: April 19, 2012Inventors: Nicole Cathleen Goodwin, Bryce Alden Harrison, Shinya Iimura, Ross Mabon, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang, Matthew Mangzhu Zhao
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Publication number: 20120040897Abstract: A compound of formula (I) or a tautomeric form, regioisomer, stereoisomer, solvate, N-oxide or pharmaceutically acceptable salts thereof; wherein ‘a’—is selected from the group consisting of substituted or unsubstituted heterocycloalkyl ring and substituted or unsubstituted carbohydrate moiety y is a member selected from —O—, —CO—, —S02-, aminoalkyl or formula (II) wherein, Rw is hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; x is a member selected from -0-, —S—, —SO—, —S02-, CONR10, NR10CO and —NRd—, or x and y together represent a chemical bond; Z is selected from —CH—, —N—. t is an integer selected from O to 4; with the provisos that when ‘a’ is substituted or unsubstituted heterocycloalkyl ring then ‘t’ is not O and when y=—CO—, x is not NRd.Type: ApplicationFiled: January 9, 2009Publication date: February 16, 2012Applicant: Sun Pharma Advanced Research Company Ltd.Inventors: Nakul Pramod Akolkar, Jay Prakashchandra Adhyapak, Javraj Dilipbhai Aradhye, Anil Savajihai Kumbhani, Bhavesh Mohanbhai Panchal, Jignesh Kantilal Jivani, Biswajit Samanta, Ranjan Kumar Pal, Rajamannar Thennati
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Patent number: 8114970Abstract: Preparation of synthetic monosaccharides, for use in the preparation of synthetic heparinoids.Type: GrantFiled: January 15, 2009Date of Patent: February 14, 2012Assignee: Alchemia LimitedInventors: Joachim Seifert, Latika Singh, Tracie E. Ramsdale, Michael L. West, Nicholas B. Drinnan
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Publication number: 20120028915Abstract: This invention relates to galactosylceramide compounds.Type: ApplicationFiled: August 2, 2011Publication date: February 2, 2012Applicants: The Scripps Reseach Institute, The University of Chicago, Brigham Young UniversityInventors: Paul B. Savage, Ablert Bendelac, Luc Teyton
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Publication number: 20110224155Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.Type: ApplicationFiled: June 3, 2008Publication date: September 15, 2011Applicant: SENOMYX INC.Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
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Publication number: 20110190230Abstract: Contemplated compositions and methods employ betalains for treatment of various conditions, and especially osteoarthritis, sinusitis, contact dermatitis, acne, an allergic condition, reduced mental alertness, reduced physical strength, reduced physical endurance, and/or impaired mood.Type: ApplicationFiled: July 30, 2009Publication date: August 4, 2011Inventor: Zbigniew Pietrzkowski
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Patent number: 7989422Abstract: The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as described herein:Type: GrantFiled: December 20, 2006Date of Patent: August 2, 2011Assignee: Alchemia LimitedInventors: Wim Meutermans, Declan McKeveney, Johannes Zuegg, Rajaratnam Premraj, Craig Muldoon, Giang Thanh Le
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Publication number: 20110117009Abstract: The present invention relates to a drug polymer conjugate comprising a pharmaceutically active compound and a dendritic polyglycerol, as well as to a drug polymer conjugate comprising a pharmaceutically and/or diagnostically active compound bound to a dendritic polyglycerol core having a polyethylene glycol shell.Type: ApplicationFiled: March 31, 2009Publication date: May 19, 2011Applicants: FREIE UNIVERSITÄT BERLIN, KTB TUMORFORSCHUNGSGESELLSCHAFT MBHInventors: Felix Kratz, Rainer Haag, Marcelo Calderon
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Publication number: 20110046003Abstract: A novel N-acetyl-5-N,4-O-carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and ?-selectivity is disclosed. Methods for making disaccharide building blocks comprising ?(2?3), ?(2?6), ?(2?8), ?(2?8)/?(2?9) alternate, and ?(2?9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutinin (HA) from various strains of influenza are provided.Type: ApplicationFiled: March 29, 2010Publication date: February 24, 2011Applicant: ACADEMIA SINICAInventors: Chi-Huey Wong, Chung-Yi Wu, Ting-Jen R. Cheng
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Patent number: 7875604Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: GrantFiled: February 1, 2005Date of Patent: January 25, 2011Assignee: University of Virginia Patent FoundationInventors: David Rekosh, Marie-Louise Hammarskjöld
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Publication number: 20100279960Abstract: The invention concerns novel biotinylated hexadecasaccharides of general formula (I) wherein: Biot is a biotin derivative; R, R1 and R2, represent independently of one another a C1-C6 alkoxy or and —OSO3; R3 represents a C1-C6 alkoxy or an —OSO3, or R3 constitutes a —O—CH2— bridge; Pe represents a saccharide concatenation; as well as their pharmaceutically acceptable salts, and their use as medicines.Type: ApplicationFiled: July 16, 2010Publication date: November 4, 2010Applicant: SANOFI-AVENTISInventors: Philippe DUCHAUSSOY, Jean Pascal HERAULT, Jean Marc HERBERT, Maurice PETITOU, Pierre SAVI
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Patent number: 7749972Abstract: The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. It is a 1-substituted-7-(?-D-glycopyranosyloxy)(aza)-indole compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof: wherein R1 represents a halogen atom or the like; n represents j an integer number from 0 to 3; R2 represents a hydrogen atom or the like; X represents a carbon atom which a hydrogen atom or the like binds to, or a nitrogen atom; Q represents an alkylene group or an alkenylene group each of which may have an oxygen atom or a sulfur atom in the chain; and A represents an aryl or heteroaryl group which may have a substituent.Type: GrantFiled: February 14, 2006Date of Patent: July 6, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Kohsuke Ohno
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Publication number: 20100121041Abstract: Disclosed is a process for producing an oxazoline derivative from a non-protected sugar in a simple manner. Also disclosed is a process for producing a glycoside by utilizing the product of the aforementioned process. A sugar oxazoline derivative is synthesized in one step in an aqueous solution from a sugar having a free hemiacetalic hydroxy group and an amido group by using a haloformamidinium derivative as a dehydrating agent. A glycoside compound is produced by using the oxazoline derivative as a sugar donor and also using a sugar dehydrogenase. The method can be applied to the production of a compound having a long sugar chain, and is therefore useful for the production of a physiologically active oligosaccharide, a carrier for a drug delivery system, a surfactant, a carbohydrate-based drug, a glycopeptide, a glycoprotein, a carbohydrate polymer or the like.Type: ApplicationFiled: March 7, 2008Publication date: May 13, 2010Inventors: Shinichiro Shoda, Atsushi Kobayashi, Masato Noguchi, Tomonari Tanaka, Hidetoshi Gyakushi
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Publication number: 20100041568Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.Type: ApplicationFiled: October 16, 2007Publication date: February 18, 2010Applicant: UNIVERSITY OF ROCHESTERInventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
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Patent number: 7655633Abstract: The present invention provides nitrogen-containing heterocyclic derivatives represented by the general formula: wherein X1 represents N or CR1; X2 represents N or CR2; X3 represents N or CR3; X4 represents N or CR4; and with the proviso that one or two of X1 to X4 represent N; R represents optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, etc.; R1 to R4 represent H, a halogen atom, etc.) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exert an excellent 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 complications, obesity or the like, pharmaceutical compositions comprising the same, and medicinal uses thereof.Type: GrantFiled: December 19, 2003Date of Patent: February 2, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masayuki Isaji
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Publication number: 20100004186Abstract: The present invention relates compounds of the formula (I) oligosaccharide-spacer-A (1), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO2—R1][CO—NR2—CH(4-benzamidine)-CO—NR3R4], 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 substituents selected from (1-8C)alkyl or (1-8C)alkoxy; and wherein R2 and R3 are independently H or (1-8C)alkyl; R4 is (?8C)alkyl or (3-8C)cycloalkyl; or R3 and R4 together with the nitrogen atom toType: ApplicationFiled: December 21, 2005Publication date: January 7, 2010Applicant: N.V. ORGANONInventors: Martin De Kort, Constant Adriaan Anton Van Boeckel
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Publication number: 20090318370Abstract: Disclosed is a novel glycoconjugated chlorin derivative which is useful as a substance for photodynamic therapy, is stable, and can act a photosensitizer having high phototoxicity even when used in a small quantity. Also disclosed is a method of producing the derivative. Specifically disclosed are a S-glycosylated chlorin derivative represented by the following general formula (1) and a metal complex thereof. In the general formula (1), X1 to X20 independently represent a group selected from the group consisting of F—, sugar-S—, sugar-Z-S— and sugar-O-Z-S— and at least one among X1 to X20 represents a group selected from the group consisting of sugar-S—, sugar-Z-S— and sugar-O-Z-S— (wherein F represents a fluorine atom, Z represents an oxygen atom, Z represents a hydrocarbon group having 1 to 6 carbon atoms); and R5 and R6 independently represent a hydrogen atom or an organic group or may together form a ring.Type: ApplicationFiled: February 12, 2008Publication date: December 24, 2009Inventors: Makoto Obata, Shigenobu Yano, Shiho Obata
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Patent number: 7566699Abstract: The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.Type: GrantFiled: March 24, 2004Date of Patent: July 28, 2009Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Shigeru Yonekubo, Hideyuki Muranaka, Hiroaki Shiohara, Hirotaka Teranishi, Kazuo Shimizu, Fumiaki Ito, Masayuki Isaji
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Publication number: 20090137499Abstract: The present invention relates to a benzylphenyl glucopyranoside derivative having an excellent inhibitory effect on human SGLT1 and/or SGLT2 activity. There is provided a compound or a pharmacologically acceptable salt thereof represented by the following general formula (I): wherein R1 represents a hydrogen atom, an amino group, a hydroxy C1-C6 alkyl group, etc.; R2 represents a hydrogen atom, etc.; R3 represents a C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, etc.; R4 represents a hydrogen atom, a C2-C7 acyl group, etc.; R5, R6, R7, and R8 are the same or different and each represents a hydrogen atom or a C1-C6 alkyl group, provided that R5, R6, R7 and R8 are not hydrogen atoms at the same time; n is 0 to 4; and X is CH or N.Type: ApplicationFiled: August 3, 2007Publication date: May 28, 2009Inventors: Takeshi Honda, Minoru Oguchi, Masao Yoshida, Ryo Okuyama, Tsuneaki Ogata, Manabu Abe, Kenjiro Ueda, Jun Ohsumi, Masanori Izumi
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Patent number: 7504489Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: December 5, 2005Date of Patent: March 17, 2009Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauve, Vern L. Schramm
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Publication number: 20090036386Abstract: Compounds and methods are provided for modulating in vitro and in vivo processes mediated by selectin binding. More specifically, selectin modulators and their use are described, wherein the selectin modulators that modulate (e.g., inhibit or enhance) a selectin-mediated function comprise glycomimetics linked to a compound, for example a member of a class of compounds termed BASAs (Benzyl Amino Sulfonic Acids) or a member of a class of compounds termed BACAs (Benzyl Amino Carboxylic Acids).Type: ApplicationFiled: May 24, 2006Publication date: February 5, 2009Applicant: GlycoMimetics, IncInventors: John L. Magnani, Arun K. Sarkar, John T. Patton, JR.
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Publication number: 20080300196Abstract: The present invention relates to monosaccharide derivatives as anti-inflammatory agents. The compounds disclosed herein can be useful for inhibition and prevention of inflammation and associated pathologies including inflammatory, cancer, cardiovascular and autoimmune diseases such as bronchial asthma, rheumatoid arthritis, type-I diabetes, multiple sclerosis, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, pruritis or allergic rhinitis. Pharmacological compositions containing compounds disclosed herein and the methods of treating diseases such as bronchial asthma, rheumatoid arthritis, type-I diabetes, multiple sclerosis, cancer, cardiovascular diseases, allograft rejection, psoriasis, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, pruritis or allergic rhinitis and other inflammatory and/or autoimmune disorders, using the compounds are also provided.Type: ApplicationFiled: October 3, 2007Publication date: December 4, 2008Inventors: Ashwani Kumar Verma, Sanjay Malhotra, Sankaranarayanan Dharmarajan, Rajkumar Shirumalla, Abhijit Ray
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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
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Patent number: 7375213Abstract: Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.Type: GrantFiled: December 23, 2003Date of Patent: May 20, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prashant P. Deshpande, Bruce A. Ellsworth, Janak Singh, Theodor W. Denzel, Chiajen Lai, Gerard Crispino, Michael E. Randazzo, Jack Z. Gougoutas
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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
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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
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Patent number: 7148223Abstract: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.Type: GrantFiled: January 31, 2005Date of Patent: December 12, 2006Assignee: Southern Research InstituteInventors: John A. Secrist, III, Kamal N. Tiwari, John A. Montgomery
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Patent number: 7129219Abstract: This invention provides compounds containing a 2-deoxy-2-amino-?-D-glucopyranose (glucosamine) glycosidically linked to a cyclic aminoalkyl (aglycon) group. The invention further provides methods for inducing an immune response using the compounds of the present invention in the presence or absence of an antigen. In addition, methods for treating disease with the compounds of the present invention with or without an antigen are also provided in this invention.Type: GrantFiled: August 3, 2001Date of Patent: October 31, 2006Assignee: Corixa CorporationInventors: David A. Johnson, C. Gregory Sowell
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Patent number: 7129220Abstract: Substituted indole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: July 30, 2004Date of Patent: October 31, 2006Assignee: Janssen Pharmaceutica N.VInventors: Mary Pat Beavers, Mona Patel, Philip Rybczynski, Maud Urbanski, Xiaoyan Zhang
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Patent number: 7112671Abstract: The present invention provides certain non-symmetric tripyrranes; that is, tripyrranes that do not contain a mirror plane of symmetry perpendicular to the plane containing the tripyrrane. Further, the invention includes texaphyrin compounds and sapphyrin compounds, as well as other polypyrrolic macrocycles, prepared using tripyrranes of Formula I as a precursor. These macrocycles are characterized by a tripyrrolic portion of the macrocyclic ring having substituents that cause the heterocycle to lack a plane of symmetry perpendicular to the plane of the macrocycle.Type: GrantFiled: August 28, 2001Date of Patent: September 26, 2006Assignee: Pharmacyclics, Inc.Inventors: Tarak D. Mody, Joshua Galanter
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Patent number: 7094764Abstract: This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.Type: GrantFiled: July 30, 2004Date of Patent: August 22, 2006Assignee: Janssen Pharmaceutica N.V.Inventor: Maud Urbanski
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Patent number: 7084124Abstract: Substituted indazole-O-glucosides, compositions containing them, and methods of using them, for example for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: July 30, 2004Date of Patent: August 1, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Mona Patel, Philip J. Rybczynski, Maud Urbanski, Xiaoyan Zhang
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Patent number: RE39245Abstract: The present invention relates to simplified synthesis, new carbohydrate-based products and practical use of different carbohydrate-based products. Examples of these are (Gal?1-3Gal), GlcNAc?1-3Gal, ?- or ?-glycosides thereof, Gal?1-3Gal- containing tri-, or higher oligosaccharides, ?- or ?-glycosides thereof, GlcNAc?1-3Gal containing tri-, tetra-, or higher oligosaccharides, and derivatives and/or ?- or ?-glycosides thereof, Gal?1-3GalGlcNAc?1-3Gal, ?- or ?-glycosides thereof, Gal?1-3Gal?1-4GlcNAc?1-3Gal?1-4Glc, or other higher oligosaccharides containing the Gal?1-3Gal-structure, ?- or ?-glycosides thereof, modified carbohydrates, di-, tri-, oligo-, or polyfunctional products containing carbohydrate structures, and the use of the products for synthesis, affinity purification, diagnostic applications and therapy.Type: GrantFiled: December 23, 1996Date of Patent: August 22, 2006Assignee: Procur ABInventor: Kurt Nilsson