Oxygen Or Sulfur Is Bonded Directly To The Carbon And Is Part Of The Chain Patents (Class 564/317)
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Publication number: 20150093365Abstract: Provided herein are compositions containing photoactivatable caged tamoxifen and tamoxifen derivative molecules. Also provided are kits containing one of these compositions and a light source. Also provided are methods of optically inducing nuclear translocation of a fusion protein containing a mammalian estrogen receptor ligand binding domain in a eukaryotic cell and methods of optically inducing recombination in a eukaryotic cell that include contacting a eukaryotic cell with at least one of these compositions. Also provided are methods of treating breast cancer in a subject that include administering a photoactivatable caged tamoxifen or tamoxifen derivative molecule to a subject having breast cancer.Type: ApplicationFiled: March 14, 2013Publication date: April 2, 2015Inventors: Xin Lu, Sarit S. Agasti, Ronald A. DePinho, Ralph Weissleder
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Patent number: 8921599Abstract: The disclosure relates to methods for producing amide bonds and reagents related thereto. In some embodiments, the disclosure relates to methods of producing an amide comprising mixing an O-silylated thionoester and an amine under conditions such that an amide is formed. In another embodiment, the disclosure relates to mixing a thiolacid, a silylating agent, and an amine under conditions such that an amide is formed.Type: GrantFiled: October 25, 2011Date of Patent: December 30, 2014Assignee: Emory UniversityInventors: Lanny S. Liebeskind, Wenting Wu, Zhihui Zhang, Hao Li, Angus A. Lamar
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Patent number: 8884061Abstract: The invention provides compounds of the formula: or a pharmaceutically acceptable salt thereof, where m, n, R1, R2, R3 R4, R5, R6, R7 are those defined herein. The invention also provides pharmaceutical compositions comprising a compound of the invention, methods for using compounds and/or pharmaceutical compositions of the invention, and methods for synthesizing compounds of the invention.Type: GrantFiled: March 2, 2007Date of Patent: November 11, 2014Assignee: Colorado State University Research FoundationInventors: Michio Kurosu, Dean Calvin Crick
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Patent number: 8865219Abstract: The invention concerns coated granules including (A) at least one amine-containing pharmacological active principle, preferably as an acid addition salt, the pharmacological active principle being complexed by low cation-exchange resin containing carboxylic acid groups (COO?), and (B) at least 15 wt. %, based on the total weight of the active principle/low cation-exchange resin complex, of at least one hydrophilic adsorbent, the mixture of the components (A) and (B) being coated with a gastrosoluble polymer. The invention also concerns a method for preparing such granules, as well as orodispesible tablets containing such granules.Type: GrantFiled: September 25, 2006Date of Patent: October 21, 2014Assignee: EthypharmInventors: Mahendra B. Chaudhari, Edouard Gendrot
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Patent number: 8461389Abstract: The invention provides a selective Sigma 1 or Dopamine D3 receptor agonist or a 5HT2c receptor ligand for use in the treatment of symptoms of anxiety and/or depression associated with an affective disorder and/or symptoms associated with cognitive impairment disorder. Particularly useful are diphenhydramine derivatives of Formula (I) and particularly (2-[(4-butylsulfanylphenyl)-phenyl-methyl]sulfanyl-N,N-dimethyl-ethanamin) (Captodiamine).Type: GrantFiled: April 20, 2009Date of Patent: June 11, 2013Assignee: University College Dublin, National University of Ireland, DublinInventors: Ciaran Regan, Lisa Conboy, Shane Gannon
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Publication number: 20130053400Abstract: The invention provides antihistamine drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the antihistamine drug not attached to the water-soluble oligomer.Type: ApplicationFiled: September 7, 2012Publication date: February 28, 2013Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang, Tacey X. Viegas, Michael D. Bentley
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Patent number: 8349899Abstract: Embodiments of the present invention comprises a compound of formula I or its enantiomer, diastereomer, stereoisomer or its pharmaceutically acceptable salt, methods of use and methods of synthesis.Type: GrantFiled: December 3, 2009Date of Patent: January 8, 2013Assignee: Arrowhead Center, Inc.Inventors: Jeffrey Arterburn, Charles Shuster
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Publication number: 20110269808Abstract: The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanok novel process intermediates and methods for making the novel process intermediates.Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITALInventors: Steven John WOODHEAD, David Charles REES, Martyn FREDERICKSON, Kyla Merriom GRIMSHAW
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Publication number: 20110160186Abstract: The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.Type: ApplicationFiled: June 9, 2009Publication date: June 30, 2011Applicant: Nektar TherapeuticsInventors: Michael A. Eldon, C. Simone Jude-Fishburn, Hema Gursahani, Myong Gyong Lee
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Publication number: 20110077581Abstract: The various embodiments of the present disclosure relate generally to compositions and methods for the targeted cellular delivery of nanoparticles. More particularly, the various embodiments of the present invention are directed to the cellular delivery of nanoparticles tethered to a ligand by way of a poly(ethylene glycol) linkage, wherein the ligand demonstrates a binding specificity for a cellular target. In an exemplary embodiment, the ligand is tamoxifen and the cellular target is the estrogen receptor, which is upregulated in many breast cancer cells.Type: ApplicationFiled: September 24, 2010Publication date: March 31, 2011Applicant: GEORGIA TECH RESEARCH CORPORATIONInventors: ADEGBOYEGA K. OYELERE, MOSTAFA A. EL-SAYED, ERIK C. DREADEN
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Publication number: 20100191475Abstract: Materials, methods and a computer system are provided which facilitate the identification and characterization of modulators of potassium ion channels, particularly the HERG channel.Type: ApplicationFiled: March 4, 2010Publication date: July 29, 2010Inventors: Scott Perschke, Ming Liu
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Publication number: 20100152201Abstract: The invention provides antihistamine drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the antihistamine drug not attached to the water-soluble oligomer.Type: ApplicationFiled: March 12, 2008Publication date: June 17, 2010Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Wen Zhang, Tacey X Viegas, Michael D Bentley
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Publication number: 20100130617Abstract: The present invention relates to new ethanolamine modulators of NMDA receptors and/or muscarinic acetylcholine receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 23, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7511070Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.Type: GrantFiled: November 9, 2005Date of Patent: March 31, 2009Assignee: Poniard Pharmaceuticals, Inc.Inventors: David J. Grainger, James C. Metcalfe, Sudhakar Kasina
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Patent number: 7126028Abstract: Process for the preparation of chiral compounds of formula (I) comprising contacting a compound of formula (II) with a source of hydrogen or halide; wherein A is a chiral center; X is selected from oxygen, sulphur and nitrogen; n is selected from 0 and 1 and is equal to the valence of X less 2; B is a fragment CR 3 2; Z is hydrogen or halogen; with the proviso that when X is nitrogen, n is 1, one of R 1 and two of R 2 are hydrogen, BZ is CHPh 2, the other R 1 and R 2 do not form together a five membered heterocyclic (pyrrolidone) ring; novel intermediates, novel compounds, polymers and libraries thereof and the use thereof as fine chemicals, and compositions thereof.Type: GrantFiled: December 6, 1999Date of Patent: October 24, 2006Assignee: The University Court of the University of St. AndrewsInventor: David O'Hagan
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Patent number: 6653508Abstract: Substituted 3-amino-2-benzyl-1-phenlypropane derivatives, methods for preparing them, pharmaceutical compositions containing them, and methods of using them to treat various medical conditions.Type: GrantFiled: January 16, 2002Date of Patent: November 25, 2003Assignee: Gruenenthal GmbHInventors: Michael Sattlegger, Helmut Buschmann, Babette-Yvonne Koegel
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Patent number: 6599921Abstract: Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyclic derivatives and have been shown to be antiproliferative against human estrogen-dependent cancer cells and to have good binding affinity for the estrogen receptor.Type: GrantFiled: August 21, 2001Date of Patent: July 29, 2003Assignee: NanoDesign, Inc.Inventors: Jonathan Martin Schmidt, Julie Mercure, Jeffry Lawrence Lowell, Stefan Kwiatkowski, Krzysztof Pupek, Shuguang Zhu, John Whelan, Natalie Lazarowych
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Patent number: 6518314Abstract: Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the composition is administered to a test animal that has received an injection of DMS, it reduces the mean volume of tissue occupied by disrupted DMS, reduces the ratio of the number of inflammatory cells per DMS, or increases the ratio of the number of macrophages containing disrupted DMS per DMS, are useful for treating cerebral amyloidosis.Type: GrantFiled: October 6, 2000Date of Patent: February 11, 2003Assignee: Nymox CorporationInventors: Paul Averback, Hossein Ghanbari, Iraj Beheshti, David Morse
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Patent number: 6414179Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.Type: GrantFiled: March 23, 2001Date of Patent: July 2, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Anne Marinier, Yonghua Gai, Serge Plamondon, Stephan Roy, Neelakantan Balasubramanian
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Publication number: 20010056210Abstract: Compounds of formula III, 1Type: ApplicationFiled: July 6, 2001Publication date: December 27, 2001Inventors: Benoit Pugin, Ivo Steiner, Rhony Niklaus Aufdenblatten, Antonio Togni
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Patent number: 6191165Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 30, 1997Date of Patent: February 20, 2001Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6172263Abstract: A method of preparing a first geometric isomer of tamoxifen or an analogue comprises allowing the first isomer to crystallize in hexanol and the product thereof to crystallize in methanol and then derivatising the product of the methanol crystallization to prepare said first isomer in very high purity.Type: GrantFiled: July 20, 1998Date of Patent: January 9, 2001Assignee: Bradford UniversityInventors: John Double, Derek Maitland, Ioana Popa
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Patent number: 6143933Abstract: A method of preparing optically active methadones comprises an enzymatic process for the resolution of 1-dialkyl-amino-2-propanol and conversion of the enantiomers to the optically active methadones in high enantiomeric purity.Type: GrantFiled: April 9, 1999Date of Patent: November 7, 2000Assignee: Salford Ultrafine Chemicals & Research Ltd.Inventors: Feodor Scheinmann, Jonathan David Hull, Nicholas John Turner
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Patent number: 6117911Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.Type: GrantFiled: April 9, 1998Date of Patent: September 12, 2000Assignee: NeoRx CorporationInventors: David J. Grainger, James C. Metcalfe, Sudhakar Kasina
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Patent number: 5773469Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.Type: GrantFiled: June 18, 1996Date of Patent: June 30, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
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Patent number: 5610183Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.Type: GrantFiled: December 17, 1993Date of Patent: March 11, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Andrew P. Owens, Brian J. Williams
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Patent number: 5521220Abstract: The present invention relates to novel acyclic ethylenediamine derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined as in the specification. It also relates to novel intermediates used in the synthesis of such derivatives.Compounds of the formula I and their pharmaceutically acceptable salts are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: July 20, 1994Date of Patent: May 28, 1996Assignee: Pfizer Inc.Inventor: Brian T. O'Neill
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Ring-substituted 2-amino-1,2,3,4-tetra-hydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes
Patent number: 5426229Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.Type: GrantFiled: December 16, 1993Date of Patent: June 20, 1995Assignee: Eli Lilly and CompanyInventors: John M. Schaus, Craig S. Hoechstetter, Diane Huser, Charles J. Paget, Robert D. Titus -
Patent number: 5192765Abstract: Amines of the following formula: ##STR1## where the variables are defined in the specification are useful in the treatment of diseases associated with altered motility and/or tone of smooth muscle.Type: GrantFiled: June 6, 1991Date of Patent: March 9, 1993Assignee: Pfizer Inc.Inventors: David Alker, Robert J. Bass, Peter E. Cross
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Patent number: 5171752Abstract: The invention relates to a benzhydryl derivative having the formula ##STR1## wherein each of the groups R.sub.1, R.sub.2, and R.sub.3 represents one to four substituents independently selected from the group consisting of hydrogen, lower alkyl, halogen, and CF.sub.3, and at least one of the groups R.sub.1, R.sub.2, and R.sub.3 is halogen or CF.sub.3 ;R.sub.4 represents hydrogen or methyl;n is 2, 3, or 4;m is 1, 2, or 3; andX represents O or S;or its pharmaceutically acceptable salts.The benzhydryl derivative of the invention can be used to treat patients who are suffering from diseases which are influenced by calmodulin.Type: GrantFiled: July 19, 1991Date of Patent: December 15, 1992Assignee: AKZO N.V.Inventors: Patricia Caldirola, Raimund Mannhold, Hendrik Timmerman
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Patent number: 4857313Abstract: The invention concerns a novel copolymer of N-morpholinoethyl methacrylate and 2-hydroxyethyl methacrylate which can be used in transdermal delivery systems or in oral controlled release products. The invention also concerns a process for preparing the copolymer and a method of using it to administer pharmaceutically active substances.Type: GrantFiled: May 28, 1987Date of Patent: August 15, 1989Assignee: Warner-Lambert CompanyInventors: Suk-zu Song, Zahra A. Rashidbaigi, Russell U. Nesbitt, Mahdi B. Fawzi
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Patent number: 4429162Abstract: The instant invention relates to compounds of the formula ##STR1## wherein each R.sub.f is independently straight or branched chain perfluoroalkyl of 2 to 18 carbon atoms or perfluoroalkoxy-perfluoroalkyl of 4 to 18 carbon atoms;each R.sub.1 is independently straight or branched chain alkylene of 1 to 12 carbon atoms, alkylenethioalkylene of 2 to 12 carbon atoms, alkyleneoxyalkylene of 2 to 12 carbon atoms, or alkyleneiminoalkylene of 2 to 12 carbon atoms where the imino nitrogen atom contains as a third substituent, hydrogen or alkyl of 1 to 6 carbon atoms;R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, chloro, bromo, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, hydroxyalkyl of 1 to 6 carbon atoms or alkoxy of 1 to 6 carbon atoms, and R.sub.2 and R.sub.3 additionally may, together with the carbon atoms to which they are attached, form a fused benzo ring;R.sub.Type: GrantFiled: February 1, 1982Date of Patent: January 31, 1984Assignee: Ciba-Geigy CorporationInventors: Thomas W. Cooke, Robert A. Falk
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Patent number: 4246201Abstract: Compound of formula: ##STR1## wherein R represents hydrogen or an alkyl group having from 1 to 4 carbon atoms; R', R", R'" and R"", equal or different from each other represent hydrogen atoms or OH groups, with the limitation that when R', R", R'" and R"" are all hydrogen atoms R cannot be an hydrogen atom and their salts with organic and inorganic pharmaceutically acceptable salts.The process for the preparation of the compounds of the above general formula are disclosed.The compounds show a good pharmacological activity and can be used as antiulcer, antispastic spasmolytic drugs.The compounds can be administered as different pharmaceutical preparations containing an effective dose of the compound in combination or in admixture with excipients suitable for oral or parenteral administration or for topical use.Type: GrantFiled: June 11, 1979Date of Patent: January 20, 1981Assignee: Alfa Farmaceutici, S.p.A.Inventor: Valerio Borzatta