Nitrogen In Aglycone Moiety Patents (Class 536/17.4)
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Publication number: 20130252910Abstract: The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH2-group, an oxygen atom, a sulphur atom, a sulfinyl group or a sulfonyl group, E is independently selected in the group comprising a hydrogen, an alkyl having from 1 to 10 carbon atoms, an aryl having from 6 to 20 carbon atoms, a nitrogen dioxide group, an azide group, an amino group, a guanidinium group, a halogen atom, a —CH2R group wherein R is a hydroxyl, a halogen, an amino group, a N(alkyl)2 group, a NH(alkyl) group, or E represents a —CO—R? wherein R? is a hydrogen atom, a hydroxyl group or an amino, B represents a A-C group wherein A is independently selected in the group comprising an oxygen atom, a sulfur atom, a NH group or a (CH2)i group, i being an integer from 1 to 10, C is independently selected in the group comprising a hydrogen, an alkyl, an alkenyl, an alkynyl, or C is a group of formula (II).Type: ApplicationFiled: December 10, 2010Publication date: September 26, 2013Inventors: Anne Imberty, Sébastien Vidal, Susan Matthews, Karine Faure, Benoit Guery, Samy Cecioni
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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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Publication number: 20130190475Abstract: The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: I wherein each of X, Alk1, Alk2, and W are as defined and described herein.Type: ApplicationFiled: July 22, 2011Publication date: July 25, 2013Applicant: SMARTCELLS, INC.Inventors: Zhiyu Chen, Thomas M. Lancaster, Todd C. Zion
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Publication number: 20130190258Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.Type: ApplicationFiled: January 24, 2013Publication date: July 25, 2013Inventors: John CASHMAN, Mark MERCOLA, Dennis SCHADE, Masanao TSUDA
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Publication number: 20130190256Abstract: The invention relates to novel curcumin derivatives in which one or two of the phenolic groups have been modified.Type: ApplicationFiled: February 25, 2011Publication date: July 25, 2013Applicant: Research Foundation of the City University of New YorkInventors: Krishnaswami Raja, Alejandra Alonso, Probal Banerjee, Sukanta Dolai, Christopher Corbo, Saadyah Averick, Amit Mogha, Shawon Debnath
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Patent number: 8492111Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 7, 2010Date of Patent: July 23, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
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Publication number: 20130184229Abstract: Compounds, compositions and methods are provided for treating cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood. More specifically, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: GLYCOMIMETICS, INC.Inventor: GlycoMimetics, Inc.
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Patent number: 8486902Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.Type: GrantFiled: October 8, 2010Date of Patent: July 16, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Adam Shilling, Argyrios G. Arvanitis, Stacey Shepard, Laurine G. Galya, Mei Li, Frank M. Nedza
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Patent number: 8486901Abstract: Novel sodium channel blocking compounds tetrodotoxm galactopyranosides of formula I were isolated and purified by HPLC and identified further through IR, NMR, GC, and MS. The compounds have a galactopyranosyl moiety attached to C11 of tetrodotoxin and retain the analgesic activity of the latter. Pharmaceutical compositions and medical uses thereof are further disclosed.Type: GrantFiled: March 26, 2010Date of Patent: July 16, 2013Assignee: Wex Medical LimitedInventor: Weiyang Lin
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Patent number: 8481696Abstract: The present invention provides novel glycopeptides antibiotic derivatives comprising a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5: Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.Type: GrantFiled: December 25, 2008Date of Patent: July 9, 2013Assignee: Shionogi & Co., Ltd.Inventors: Kouhei Matsui, Kazuyuki Minagawa, Osamu Yoshida, Kenji Morimoto, Yuuki Ogata
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Patent number: 8470786Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 23, 2011Date of Patent: June 25, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Darin Kizer, Takahiro Murai, Daisuke Nakai, Takanori Yasukochi
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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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Publication number: 20130142757Abstract: Disclosed are compounds of general formula (I), wherein R, R1, Rc, Rd, Re, Rf, X, Y, Z, A and B are as defined in the application.Type: ApplicationFiled: May 23, 2011Publication date: June 6, 2013Applicants: Hande Starlake Bioscience Co., Ltd., Hande Pharma LimitedInventors: Chenxi LI, Weisheng Shen, Yang Fang, Xiaoyong Le
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Publication number: 20130144045Abstract: The present invention relates to a compound of general formula (I): in which: X is OH, NH2, NHOH or RNH, where R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, Y is H, or an electron-withdrawing group, in particular selected from NO2, CF3 or a halogen, R1 and R2 are H or a linear or branched, saturated or unsaturated, C1-C10 alkyl radical, F is a reactive functional group that can be activated by click chemistry.Type: ApplicationFiled: May 18, 2011Publication date: June 6, 2013Applicants: UNIVERSITE DE POITIERS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Sebastien Papot, Mickael Thomas
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Patent number: 8450466Abstract: One aspect of the present invention relates to compounds, compositions and methods for diagnosis and/or treatment of a subject suffering from an amyloidosis-associated pathological condition. In certain embodiments, the imaging and/or therapeutic agents of the instant invention may be administered to a subject for identification and/or treatment of amyloid deposits. A specific imaging method detects amyloid deposits by administering the imaging agent to the subject and detecting the spatial distribution of the agent. Differential accumulation of the agent is indicative of AD or an amyloidosis-associated pathological condition and can be monitored by using a PET or SPECT camera.Type: GrantFiled: March 23, 2009Date of Patent: May 28, 2013Assignees: The General Hosptial Corporation, Fluoropharma, Inc.Inventors: David R. Elmaleh, Timothy M. Shoup, Hongning Fu
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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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Publication number: 20130116417Abstract: Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative.Type: ApplicationFiled: June 10, 2011Publication date: May 9, 2013Applicant: BRANDEIS UNIVERSITYInventors: Isaac J. Krauss, Lizbeth K. Hedstrom, Iain S. MacPherson
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Publication number: 20130116203Abstract: The present invention provides glucosinolate and isothiocyanate compounds and related methods for synthesizing these compounds and analogs. In certain embodiments, these glucosinolate and isothiocyanate compounds are useful and chemopreventive and or chemotherapeutic agents.Type: ApplicationFiled: November 7, 2011Publication date: May 9, 2013Inventors: Scott R. Rajski, Jared Rae Mays
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Publication number: 20130116204Abstract: Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.Type: ApplicationFiled: December 21, 2010Publication date: May 9, 2013Applicant: Celgene CorporationInventors: Peter H. Schafer, Anthony J. Frank, Hon-Wah Man, Sai L. Shankar
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Publication number: 20130102049Abstract: Novel method and reagents for generating reversibly tagged saccharides, aldehydes, carboxyl acids, or orthoacetates useful in analytical and diagnostic applications are disclosed. Saccharides are coupled at the reducing end to tagging moieties comprising a reagent selected from a ortho-diaminobenzoic(DAB)-peptide, an aldo-imidazole or N-methylated aldo-imidazole, or an ortho-phenyldiamine (OPD) or substituted OPD. The tagged saccharide further comprising detectable or functional groups coupled to the tagging moiety are provided. Kits and reagents for chromatography and mass spectrometry are disclosed.Type: ApplicationFiled: July 12, 2012Publication date: April 25, 2013Applicant: ACADEMIA SINICAInventor: Wen-Bin YANG
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Publication number: 20130095548Abstract: Derivatives of PSAs are synthesised, in which a reducing and/or non-reducing end terminal sialic acid unit is transformed into a N-hydroxysuccinimide (NHS) group. The derivatives may be reacted with substrates, for instance substrates containing amine or hydrazine groups, to form non-cross-linked/crosslinked polysialylated compounds. The substrates may, for instance, be therapeutically useful drugs, peptides or proteins or drug delivery systems.Type: ApplicationFiled: July 9, 2012Publication date: April 18, 2013Inventors: Sanjay JAIN, Ioannis PAPAIOANNOU, Smita THOBHANI
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Publication number: 20130072449Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: August 14, 2012Publication date: March 21, 2013Applicant: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8399418Abstract: 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 bis[3-(3-{4-[3-(?-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide]monosebacate 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: December 24, 2008Date of Patent: March 19, 2013Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Hideki Takeuchi, Eiji Tsuru
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Patent number: 8394774Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.Type: GrantFiled: February 11, 2010Date of Patent: March 12, 2013Assignee: Dow AgroSciences, LLC.Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Annette V. Brown, Thomas L. Siddall
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Publication number: 20130060014Abstract: A surface-modified inorganic material and a preparation method thereof. A surface-modified inorganic material is provided which is obtained by allowing an organosilane compound having allyl or an allyl derivative to react with an inorganic material, particularly solid silica or ITO glass, in the presence of an acid and an organic solvent, to introduce an organic group into the inorganic material even at room temperature, as well as a preparation method thereof. The invention can effectively introduce the organic group into the inorganic material even at room temperature, and thus is very effective in introducing compounds having a thermally sensitive functional group, for example, natural compounds or proteins. It is possible to introduce various organic groups into an inorganic material and to separate and purify organic molecule-bonded organosilane compounds using a silica gel column to effectively bond them to inorganic materials.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventors: Chul-Ho Jun, Ye-Lim Yeon, Ji-Sung Lee, Young-Jun Park
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Patent number: 8389698Abstract: A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.Type: GrantFiled: June 26, 2009Date of Patent: March 5, 2013Assignee: Wyeth LLCInventors: Li Shen, Kelly Keating, Oliver McConnell, William DeMaio, Appavu Chandrasekaran
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Publication number: 20130053334Abstract: The invention features compounds of formula (V) or(XII). In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.Type: ApplicationFiled: January 28, 2011Publication date: February 28, 2013Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Narayanannair K. Jayaprakash, Kallanthottahil G. Rajeev, Michael E. Jung
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Patent number: 8383786Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. A compound having the following structure is disclosed.Type: GrantFiled: February 11, 2010Date of Patent: February 26, 2013Assignee: Dow AgroSciences, LLC.Inventors: Gary D. Crouse, Thomas C. Sparks, CaSandra Lee McLeod, David A. Demeter, Zoltan L. Benko, Debra L. Camper
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Publication number: 20130039904Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.Type: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
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Publication number: 20130019348Abstract: This document discloses molecules having the following formula (“Formula One”) The molecules disclosed in this document are related to the field of processes to produce molecules that are useful as pesticides (e.g., acaricides, insecticides, molluscicides, and nematicides), such molecules, and processes of using such molecules to control pests.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, David A. Demeter, Thomas C. Sparks, Nick X. Wang, William H. Dent, III, Carl Deamicis, Noormohamed M. Niyaz, Erich W. Baum, Lindsey G. Fischer, Natalie C. Giampietro
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Publication number: 20130018179Abstract: This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.Type: ApplicationFiled: September 21, 2012Publication date: January 17, 2013Applicant: WYETH LLCInventors: Keith MORAN, Jianxin GU
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Publication number: 20130017162Abstract: The invention relates to a cosmetic composition, especially a hair composition, and to a method for the cosmetic treatment of keratin materials, especially of the hair, employing compounds of formula: in which Z represents (i) a hydrogen atom, (ii) a linear or branched C1 to C32 (saturated) alkyl radical; (iii) a linear or branched C2 to C32 (unsaturated) alkene radical, comprising one or two C?C double bonds; (iv) an aryl-substituted alkyl radical; said radicals being optionally substituted and/or interrupted.Type: ApplicationFiled: January 4, 2011Publication date: January 17, 2013Applicant: L'OREALInventors: Anne-Claude Dublanchet, Christian Blaise, Abel Messavussu
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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: 20130012464Abstract: The present invention provides a pharmaceutically acceptable compound, a pharmaceutical composition comprising the above-mentioned pharmaceutically acceptable compound. The pharmaceutically acceptable compound provided by the present invention is a salt of a basic group-containing morphinan derivative and a carboxyl group-containing glycyrrhizinic acid and has the ability to be used to manufacture medicaments for treating and/or preventing cough, ameliorating pains, treating respiratory system diseases, treating cardiovascular diseases and treating liver diseases.Type: ApplicationFiled: July 7, 2011Publication date: January 10, 2013Inventors: Chin-Tsai FAN, Cheng-Shun Lai, Wen-Yen Yeh, Yu-Ying Liu
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Publication number: 20130012467Abstract: The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human ?-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by ?-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC50=1080 nM) but could be activated by ?-glucuronidase to display potent activity (IC50=13.3 nM).Type: ApplicationFiled: November 24, 2010Publication date: January 10, 2013Applicant: Academia SinicaInventors: Zeljko M. Prijovic, Yu-Lin Leu, Steve R. Roffler
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Publication number: 20130012692Abstract: The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: ApplicationFiled: June 8, 2012Publication date: January 10, 2013Applicant: Parion Sciences, Inc.Inventor: MICHAEL R. JOHNSON
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Publication number: 20120329743Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: June 14, 2012Publication date: December 27, 2012Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
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Publication number: 20120322974Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.Type: ApplicationFiled: March 13, 2012Publication date: December 20, 2012Applicant: University of Georgia Research Foundation, Inc.Inventors: GEERT-JAN BOONS, Jun Guo, Xinghai Ning, Margaretha Wolfert
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Publication number: 20120309701Abstract: The present invention encompasses compounds and methods for treating urinary tract infections.Type: ApplicationFiled: April 23, 2012Publication date: December 6, 2012Applicant: THE WASHINGTON UNIVERSITYInventors: James W. Janetka, Zhenfu Han, Scott Hultgren, Jerome S. Pinkner, Corinne Cusumano
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Patent number: 8324176Abstract: 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 an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.Type: GrantFiled: April 9, 2009Date of Patent: December 4, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
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Publication number: 20120295860Abstract: The present invention relates to a compound The instant invention relates to a compound of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B), wherein R? represents and R? represents hydrogen, hydroxy, C1-C7alkoxy, C1-C8-alkanoyloxy, or R5R4N—CO—O—, where R4 and R5 independently are C1-C7alkyl or phenyl which is unsubstituted or substituted by a substitutent selected from C1-C7alkyl, C1-C7alkoxy, halogen and trifluoromethyl and where R4 additionally is hydrogen; or R4 and R5 together represent C3-C6alkylene, in free form or in form of a pharmaceutically acceptable acid addition salt. Compounds of formulae (I A), (I B), (X A), (X B), (Y A) or (Y B) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.Type: ApplicationFiled: July 27, 2012Publication date: November 22, 2012Inventors: Ulrich Hassiepen, Matthias Kittelmann
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Publication number: 20120295866Abstract: The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs. This invention relates to a method for the production of a broad group of glycosylated drugs, including but not limited to propofol, acetaminophen, and camptothecin carbohydrate derivatives.Type: ApplicationFiled: April 9, 2012Publication date: November 22, 2012Inventors: Brian Shull, John Baldwin, Ramesh Gopalaswamy, Zishan Haroon
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Patent number: 8314071Abstract: Certain aspects of the invention relate to antibiotics, as well as pharmaceutically acceptable salts, pro-drugs and/or analogs thereof. Another aspect of the invention relates to methods of use of said antibiotics.Type: GrantFiled: December 22, 2008Date of Patent: November 20, 2012Assignee: Massachusetts Institute of TechnologyInventors: Anthony J. Sinskey, Philip A. Lessard, Kazuhiro Kurosawa
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Publication number: 20120283209Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: April 6, 2012Publication date: November 8, 2012Applicant: Achaogen, Inc.Inventors: Paola Dozzo, Adam Aaron Goldblum, James Bradley Aggen, Martin Sheringham Linsell
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Publication number: 20120270824Abstract: Compounds of the formula (I) wherein n is 0, 1 or 2, R1 is aryl, heteroaryl or heterocyclyl, and R2 and R3 are hydrogen or a substituent as described in the specification, are useful for the prevention and treatment of bacterial infections, in particular of urinary infections caused by E. coli.Type: ApplicationFiled: December 13, 2010Publication date: October 25, 2012Inventors: Beat Ernst, Janno Herold
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Publication number: 20120270819Abstract: Use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases The invention relates to the use of compounds with SGLT-1/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases like osteoporosis. Preferred is the use of compounds of the formula I in which the radicals have the stated meanings.Type: ApplicationFiled: October 1, 2010Publication date: October 25, 2012Applicant: SANOFIInventors: Thomas Kissner, Martin Heinrichs, Eckart Krupp
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Publication number: 20120269766Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H? function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.Type: ApplicationFiled: October 12, 2010Publication date: October 25, 2012Applicant: Yale UniversityInventors: David Spiegel, Christopher Parker
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Publication number: 20120263625Abstract: Antimicrobial molecular conjugates for the treatment and prevention of infectious diseases caused by pathogenic microorganisms in human and animals are provided. The key to these conjugates is connecting dihydroxychlorins or ?-functionalized chlorins to carbohydrate moieties. These conjugates are found to be very effective in combating bacterial infections caused by Gram-positive and Gram-negative bacteria, including their resistant strains. Significantly, they are also effective in complex environments, including blood, serum, and other body fluids which are present in patient's body. A method of use to control pathogenic microorganisms in human and animals is also provided.Type: ApplicationFiled: July 22, 2011Publication date: October 18, 2012Inventors: Daniel Aicher, Volker Albrecht, Burkhard Gitter, Christian B. W. Stark, Arno Wiehe
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Publication number: 20120264925Abstract: A process for preparing pyrazole-glycoside derivatives of the general Formula (I) in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl, where one, more than one or all hydrogen(s) may be replaced by fluorine; X (C1-C3)-alkylene, (C2-C3)-alkenylene.Type: ApplicationFiled: August 26, 2010Publication date: October 18, 2012Applicant: SANOFIInventors: Michael Podeschwa, David Rigal, Kai Rossen, Bernhard Otto, Hermut Wehlan, Theodor Andreas Wollmann, Bernd Becker, Berndt Kulitzscher, Alexander Schaefer