The Hetero Ring Is Five-membered And Has Plural Hetero Atoms Patents (Class 540/108)
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Patent number: 10385093Abstract: Compounds useful for molecular imaging of cells expressing estrogen receptors are provided. Also provided are intermediates for making the compounds and methods of making the compounds using a modular convergent strategy. Further, methods of making the intermediates are described, as well as methods of diagnosing disease in a subject by using the compounds as imaging agents.Type: GrantFiled: December 10, 2013Date of Patent: August 20, 2019Assignee: Northeastern UniversityInventors: Robert N. Hanson, Kinh-Luan Dao
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Patent number: 9642804Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.Type: GrantFiled: October 6, 2015Date of Patent: May 9, 2017Assignee: SIRNA THERAPEUTICS, INC.Inventors: Mark Cameron, Jennifer R. Davis, Andrea R. Geiser, Matthew G. Stanton, Vladislav V. Telyatnikov, Lu Tian, Weimin Wang
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Patent number: 9447141Abstract: The present invention relates to a process for the preparation of sterol derivatives comprising the reaction of an ?-epoxy compound with an amine in an alcohol comprising 3 to 5 carbon atoms as a solvent.Type: GrantFiled: November 23, 2012Date of Patent: September 20, 2016Assignee: (INSERM) (Institut National de la Sante et de la Recherche Medicale)Inventors: Marc Poirot, Michael Paillasse, Philippe De Medina, Sandrine Poirot
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Patent number: 9402912Abstract: The present invention describes novel single drug entities, formed by direct linkage of an antibiotic to a steroidal drug. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs. The antibiotic is coupled directly to the steroid drug.Type: GrantFiled: March 6, 2014Date of Patent: August 2, 2016Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Ken Chow, Liming Wang, Michael E. Garst, Mayssa Attar, Brandon D. Swift
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Patent number: 8940719Abstract: Certain chemical entities chosen from compounds of Formula I: and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof are described. Pharmaceutical compositions comprising at least one chemical entity chosen from compounds of Formula I and a pharmaceutically acceptable vehicle are described. Also described are methods for inhibiting ?-2,3-sialyltransferase activity in cells, and methods for treating a patient having a disease responsive to inhibition of ?-2,3-sialyltransferase activity.Type: GrantFiled: July 3, 2006Date of Patent: January 27, 2015Assignee: Academia SinicaInventors: Wen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
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Publication number: 20140378673Abstract: Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.Type: ApplicationFiled: February 13, 2013Publication date: December 25, 2014Inventors: Yukio Nagasaki, Yutaka Ikeda, Hikaru Hisano
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Publication number: 20140364600Abstract: Described herein are imidazolyl compounds which either act as pure antiprogestins and methods of using such pure antagonists for gynecological indications and breast cancer.Type: ApplicationFiled: June 5, 2013Publication date: December 11, 2014Inventors: Klaus Nickisch, Walter Elger, Bindu Santhamma
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Publication number: 20140356322Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
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Patent number: 8884022Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: GrantFiled: January 4, 2013Date of Patent: November 11, 2014Assignee: North Carolina State UniversityInventors: Christian Melander, Steven A. Rogers
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Publication number: 20140288160Abstract: Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent transfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids.Type: ApplicationFiled: June 8, 2012Publication date: September 25, 2014Applicant: Shire Human Genetic Therapies, Inc.Inventors: Braydon Charles Guild, Michael Heartlein, Frank DeRosa, Jerry Chi Zhang
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Patent number: 8841284Abstract: There is provided a novel compound having neurite-outgrowing activity that is useful for the prevention or the treatment of a neurodegenerative disease. A compound of Formula (I) [where X is OR or NR1R2, Y is OH, NR3R4, —NHC(?NH)NHR5, or —NHC(?NH)R5, and Z is a hydrogen atom, a linear or branched C1-5 alkyl group, or a 5- or 6-membered ring aryl group optionally having 1 or 2 nitrogen atom(s), sulfur atom(s), or oxygen atom(s)], or a pharmaceutically or veterinary-medically acceptable salt of the compound.Type: GrantFiled: July 21, 2009Date of Patent: September 23, 2014Assignee: Lead Chemical Co., LtdInventors: Hideo Nemoto, Yuji Matsuya
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Patent number: 8843126Abstract: A programmable device generates a test signal indicative of a RF signal and receives a processed test signal indicative of the test signal after processing thereof by one of a RF transmission system and a RF receiving system. The programmable device performs a comparison between the processed test signal and calibration data, and generates a report based on the comparison. A hardwire signal router provides the test signal to one of the RF transmission system and the RF receiving system, and provides the processed test signal to the programmable device. The router includes a first switching mechanism and a second switching mechanism operating in a coordinated fashion to define one of a first state for testing the RF transmission system and a second state for testing the RF receiving system.Type: GrantFiled: August 3, 2012Date of Patent: September 23, 2014Assignee: The United States of America as represented by the Secretary of the NavyInventor: Curtis Z. Richard
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Publication number: 20140194620Abstract: The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.Type: ApplicationFiled: May 11, 2012Publication date: July 10, 2014Applicant: FUTURECHEM CO., LTD.Inventors: Dae-Yoon Chi, Byoung-Se Lee, Chansoo Park, Min-Hyung Lee, Hyojin Cha, Woojin Cho, Heewon Kang, Kyunghun Kim
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Publication number: 20140005156Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)Inventors: MARC POIROT, PHILIPPE DE MEDINA, SANDRINE POIROT
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Publication number: 20140005132Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.Type: ApplicationFiled: July 1, 2013Publication date: January 2, 2014Applicants: REGENTS OF THE UNIVERSITY OF MINNESOTA, THE UNIVERSITY OF KANSASInventors: Gustavo Blanco, Gunda I. Georg, Shameem Sultana Syeda
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Publication number: 20130336996Abstract: A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of the conjugated compound, as well as a complex formed between the conjugated compound and a polyanionic molecule and a pharmaceutical composition containing the conjugated compound or complex. Also described is the use of the conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.Type: ApplicationFiled: March 15, 2013Publication date: December 19, 2013Applicant: CAYLAInventors: Fabienne VERNEJOUL, Arnaud DEBIN, Daniel DROCOURT, Eric PEROUZEL, Gerard TIRABY, Thierry LIOUX
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Publication number: 20130156705Abstract: Bivalent multifunctional A? oligomerization inhibitors (BMAOIs) that target multiple risk factors involved in Alzheimer's disease are provided. The BMAOIs are useful for the treatment and/or prevention of Alzheimer's disease, as well as for diagnostic imaging of A? plaques in brain tissue. The BMAOIs comprise i) an A? oligomer (ApO)-inhibitor moiety which may have antioxidant activity (e.g. curcumin, curcumin derivatives, curcumin hybrids, resveratrol, etc.); ii) a cell membrane/lipid raft (CM/LR) anchoring moiety (e.g. cholesterol, cholesterylamine, a steroid, etc.Type: ApplicationFiled: July 14, 2011Publication date: June 20, 2013Applicant: Virginia Commonwealth UniversityInventors: Shujin Zhang, Tai Liang Guo
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Publication number: 20130123225Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Inventor: North Carolina State University
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Patent number: 8435973Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.Type: GrantFiled: September 28, 2010Date of Patent: May 7, 2013Assignee: Abbott Products GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
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Patent number: 8361996Abstract: The present invention provides a novel series of imidazolyl substituted steroidal and indan-1-one derivatives and salts thereof having the following general structural formulae (A and B)Type: GrantFiled: September 8, 2006Date of Patent: January 29, 2013Assignee: Council of Scientific and Industrial ResearchInventors: Ranju Bansal, Sheetal Guleria, Gaurav Narang, Rolf Wolfgang Hartmann
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Publication number: 20120316145Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-benzylidene derivatives of the formula I, in which Y and X are each as defined in the claims and the description, to a process for preparation thereof and to the use thereof as medicaments.Type: ApplicationFiled: July 7, 2010Publication date: December 13, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
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Publication number: 20120258941Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.Type: ApplicationFiled: July 8, 2010Publication date: October 11, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
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Publication number: 20120238740Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.Type: ApplicationFiled: July 6, 2010Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Keith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
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Publication number: 20120232042Abstract: The invention relates to 17-hydroxy-13-methyl-17-pentafluoroethyl-11-acyloxyalkylenephenyldodecahydrocyclopenta[a]phenanthren-3-one derivatives of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.Type: ApplicationFiled: July 7, 2010Publication date: September 13, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Moller, Andrea Rotgeri, Ursula Krenz
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Publication number: 20120190660Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-ethynylphenyl derivatives of the formula I, in which R1 and X are each as defined in the claims and the description, and to a process for preparation thereof and to the use thereof as medicaments.Type: ApplicationFiled: July 8, 2010Publication date: July 26, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
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Publication number: 20120184515Abstract: The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene-11-methyleneoxyalkylenearyl derivative of the formula I with progesterone-antagonising action and to processes for preparation thereof, to use thereof for treatment and/or prophylaxis of disorders and to the use thereof for production of medicaments for treatment and/or prophylaxis of disorders, especially of fibroids of the uterus (myomas, uterine leiomyomas), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause, or for fertility control and emergency contraception.Type: ApplicationFiled: July 7, 2010Publication date: July 19, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Klar, Wolfgang Schwede, Carsten Möller, Andrea Rotgeri, Wilhelm Bone
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Publication number: 20120115169Abstract: Provided is a derivative of 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol. Also provided is a protein conjugated to the above derivative. Further provided is an antibody composition comprising antibodies that specifically bind to 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol. Additionally, a method of making antibodies that specifically bind to 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol is provided. Also, a method of assaying for 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol is provided. Additionally provided is a kit for detecting 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol.Type: ApplicationFiled: November 9, 2010Publication date: May 10, 2012Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.Inventors: Michael C. Mullenix, Robert Elliot Zipkin, Jeffrey Kroll Adams, Wayne Forrest Patton, James J. Donegan
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Publication number: 20120046461Abstract: Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.Type: ApplicationFiled: January 25, 2010Publication date: February 23, 2012Applicant: Northeastern UniversityInventor: Robert N. Hanson
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Patent number: 8119619Abstract: Steroid compounds possessing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.Type: GrantFiled: January 7, 2011Date of Patent: February 21, 2012Assignee: Umecrine ABInventors: Torbjörn Bäckström, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
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Patent number: 8080540Abstract: Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: GrantFiled: September 18, 2007Date of Patent: December 20, 2011Assignee: Abbott Products GmbHInventors: Josef Messinger, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Lila Kallio nee Pirkkala
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Publication number: 20110262368Abstract: The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activity. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.Type: ApplicationFiled: December 18, 2008Publication date: October 27, 2011Applicant: Schering CorporationInventors: John C. Anthes, Kevin D. McCormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Daniel M. Solomon, Philippa H. Solomon, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar
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Patent number: 7960367Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.Type: GrantFiled: December 20, 2002Date of Patent: June 14, 2011Assignee: Umecrine ABInventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
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Patent number: 7947668Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.Type: GrantFiled: April 18, 2003Date of Patent: May 24, 2011Assignee: Institut National de la Sante et de la Recherche MedicaleInventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
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Patent number: 7888340Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.Type: GrantFiled: December 20, 2002Date of Patent: February 15, 2011Assignee: Umecrine ABInventors: Torbjorn Backstrom, Per Lundgren, Ming-De Wang, Inga-Maj Johansson
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Patent number: 7687486Abstract: Compositions and methods for treating a cancer in mammals by administering selective estrogen receptor modulators particularly compounds represented by: or any other of the structures contained herein, or of a stereoisomer, enantiomer, rotomer, tautomer or pharmaceutically acceptable salt form thereof.Type: GrantFiled: March 5, 2005Date of Patent: March 30, 2010Assignee: Florida Agricultural & Mechanical UniversityInventor: John S. Cooperwood
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Patent number: 7671045Abstract: The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.Type: GrantFiled: February 16, 2007Date of Patent: March 2, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Weiqin Jiang, Zhihua Sui
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Publication number: 20100048888Abstract: The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.Type: ApplicationFiled: October 17, 2007Publication date: February 25, 2010Inventors: Tongqian Chen, Kurt Vagle, Chandra Vargeese, Weimin Wang, Ye Zhang
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Publication number: 20090137541Abstract: The present invention provides a novel series of imidazolyl substituted steroidal and indan-1-one derivatives and salts thereof having the following general structural formulae (A and B)Type: ApplicationFiled: September 8, 2006Publication date: May 28, 2009Inventors: Ranju Bansal, Sheetal Guleria, Gaurav Narang, Rolf Wolfgang Hartmann
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Publication number: 20090105202Abstract: The disclosure provides androsterone derivatives. The derivatives of the disclosure are useful in the treatment of androgen- and estrogen-associated diseases and disorders, including breast cancer.Type: ApplicationFiled: October 18, 2006Publication date: April 23, 2009Applicants: CALIFORNIA PACIFIC MEDICAL CENTER, CATHOLIC HEALTHCARE WESTInventor: Li-Xi Yang
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Patent number: 7407947Abstract: An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9, together with liposomes containing such compounds and their uses.Type: GrantFiled: February 21, 2002Date of Patent: August 5, 2008Assignee: Novosom AGInventors: Steffen Panzner, Gerold Endert, Stefan Fankhaenel, Nasr El-Mokdad
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Publication number: 20080146531Abstract: Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring the inhibition of a 17?-hydroxysteroid dehydrogenase (17?-HSD) such as 17?-HSD type 1, type 2 or type 3 enzyme.Type: ApplicationFiled: September 18, 2007Publication date: June 19, 2008Applicant: SOLVAY PHARMACEUTICALS GmbHInventors: Josef Messinger, Uwe Schoen, Heinrich-Hubert Thole, Bettina Husen, Pasi Koskimies, Lila KALLIO nee Pirkkala
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Patent number: 7312206Abstract: Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also relates to liposomes containing said sterol derivatives.Type: GrantFiled: February 21, 2002Date of Patent: December 25, 2007Assignee: Novosom AGInventors: Steffen Panzner, Gerold Endert, Stefan Fankhänel, Anja Behrens
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Patent number: 6984634Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.Type: GrantFiled: October 9, 2001Date of Patent: January 10, 2006Assignee: XenoPort, Inc.Inventors: Kenneth C. Cundy, Mark A. Gallop
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Patent number: 6953785Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 24, 2001Date of Patent: October 11, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Tsutomu Agatsuma, Kozue Muramatsu, Takeshi Takahashi, Shiro Akinaga, Chikara Murakata
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Patent number: 6921757Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticalsType: GrantFiled: June 26, 2001Date of Patent: July 26, 2005Assignee: Novartis AGInventors: Bernard Cuenoud, David Beattie, Thomas Hugo Keller, Gaynor Elizabeth Pilgrim, David Andrew Sandham, Simon James Watson
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Patent number: 6878698Abstract: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof together with a long-acting ?2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of COPD over a period of 24 hours or more.Type: GrantFiled: October 28, 2002Date of Patent: April 12, 2005Assignee: Glaxo Group LimitedInventors: Keith Biggadike, Paul Spencer Jones, Jeremy John Payne
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Patent number: 6740645Abstract: The invention is directed to a novel class of 17&bgr;-acyl-17&agr;-propynyl steroids which exhibit potent antiprogestational activity.Type: GrantFiled: September 3, 1999Date of Patent: May 25, 2004Assignee: Research Triangle InstituteInventors: C. Edgar Cook, John A. Kepler, Jill M. O'Reilly
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Patent number: 6566542Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as in the specification.Type: GrantFiled: June 18, 2002Date of Patent: May 20, 2003Assignee: Aventis Pharma S.A.Inventors: Yasmina Bouali, Jacques Mauger, Patrick Van De Velde, Francois Nique
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Patent number: 6537983Abstract: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and {overscore (-----)} represents a single or a double bond; and salts and solvates thereof together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.Type: GrantFiled: February 4, 2002Date of Patent: March 25, 2003Assignee: SmithKline Beecham CorporationInventors: Keith Biggadike, Paul Spencer Jones, Jeremy John Payne
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Patent number: 6509462Abstract: The present invention provides a highly sensitive immunoassay system for estrogens, which utilizes as a labeled compound a biotinylated estradiol derivative of the formula (1) wherein one of R1 and R2 is hydrogen and the other is a group represented by wherein R3s are the same or different and represent an arginine residue or a lysine residue, x is 0 or 1, y is an integer from 1 to 5, and z is an integer from 1 to 3.Type: GrantFiled: July 17, 2001Date of Patent: January 21, 2003Assignees: Otsuka Pharmaceutical Co., Ltd., Yanaihara Institute, Inc.Inventors: Noboru Yanaihara, Ikuo Kato, Kazuyuki Kitamura, Tsukasa Kodaira