Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/402)
-
Patent number: 11726026Abstract: A method and system for early detection of biofouling utilizing a fluorescence based extracellular enzyme activity assay is disclosed. The method provides a means for early detection of biofouling on membranes used in flow-through membrane filtration systems for with a feed water flow, such as waste water of water for desalination. Also disclosed is an at-line sensor utilizing the fluorescence based extracellular enzyme activity assay that is positioned in the membrane filtration system for detection of biofouling.Type: GrantFiled: August 21, 2017Date of Patent: August 15, 2023Assignee: KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Babar Khalid Khan, TorOve Leiknes
-
Patent number: 10471054Abstract: Provided is a series of acetyl Chrysin Mannich base derivatives with the structures illustrated in the following scheme: wherein R1 is acetyl and R2 is cycloalkylamine-methyl, or R2 is acetyl and R1 is cycloalkylamine-methyl. Such derivatives are cyclin-dependent protein kinases 1 (CDK1) selective inhibitors. Base on the levels of .O2? and Fe++ are higher 5-15 times in cancer cells than in normal cells, the action mechanism of such derivatives by regulating intracellular reactive oxygen species (ROS) is activating mitochondria apoptosis pathway without the death receptor pathway, thus selectively inducing apoptosis of cancer cells and protecting normal cells. Inside, CH-j has a good druggability for the selectivity of solid cancers. Moreover, CH-f has also a good druggability for the systemic cancers.Type: GrantFiled: December 13, 2018Date of Patent: November 12, 2019Inventor: Fan Zhang
-
Patent number: 10442783Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: November 3, 2010Date of Patent: October 15, 2019Assignee: RHIZEN PHARMACEUTICALS SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V. S. Vakkalanka
-
Patent number: 9512064Abstract: Mew tranilast complexes and new tranilast cocrystais are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.Type: GrantFiled: March 29, 2013Date of Patent: December 6, 2016Assignee: NUFORMIX LIMITEDInventors: Joanne Holland, Christopher Frampton
-
Patent number: 9233169Abstract: The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: GrantFiled: February 20, 2015Date of Patent: January 12, 2016Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
-
Patent number: 9095621Abstract: The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: GrantFiled: April 23, 2009Date of Patent: August 4, 2015Assignee: NEKTAR THERAPEUTICSInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
-
Patent number: 8716497Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: September 10, 2012Date of Patent: May 6, 2014Assignees: Children's Hospital Medical Center, Ausio Pharmaceuticals, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
-
Patent number: 8686154Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: June 10, 2009Date of Patent: April 1, 2014Assignee: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
-
Patent number: 8673966Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I: which are ALDH-2 inhibitors, useful for treating a patient in need thereof, for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.Type: GrantFiled: August 30, 2012Date of Patent: March 18, 2014Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani, Jeff Zablocki
-
Patent number: 8629197Abstract: A chemically patterned modified hydrogel formed from a modified hydrogel is provided. The hydrogel is conjugated with a multiphoton photocleavable molecule. The molecule has a multiphoton-labile protective group and a protected group. The protective group is cleavable upon multiphoton excitation to deprotect the protected group, without substantial polymerization of the hydrogel. The chemically patterned modified hydrogel is formed by exposing the modified hydrogel to multiphoton excitation to deprotect a portion of the protected groups.Type: GrantFiled: April 7, 2008Date of Patent: January 14, 2014Inventors: Molly Shoichet, Jordan Wosnick, Ryan Wylie
-
Patent number: 8461198Abstract: This invention provides a method for treating or preventing human atrial arrhythmia (fibrillation) using the leading flavone compound acacetin, and its derivatives and analogues that inhibit the ultra-rapidly-activating delayed rectifier potassium current (IKur or IKsus), transient outward potassium (Ito), and acetylcholine-activated potassium current (IK.Ach).Type: GrantFiled: September 7, 2010Date of Patent: June 11, 2013Assignees: Versitech Limited, Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Gui-Rong Li, Chu-Pak Lau, Guo-Wei Qin, Hong-Bing Wang
-
Publication number: 20130137694Abstract: There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions.Type: ApplicationFiled: May 31, 2011Publication date: May 30, 2013Inventors: Gerald Batist, Jian Hui Wu
-
Publication number: 20130030009Abstract: A method of applying a topical preparation of at least one of a mast cell stabilizer, an antihistamine, and a leukotriene inhibitor is disclosed for prevention and/or treatment of oral allergy syndrome of the lips, including lip itchiness and/or swelling. For example, topical application of Cromolyn Sodium to the lips can be used to prevent and/or treat allergic reaction to consumption or other contact with raw fruits and/or raw vegetables. The topical administration can be performed by using applicator devices that apply at least one of a mast cell stabilizer and an antihistamine in the form of a liquid, or a gel, or a butter, or a wax-like solid, or a liposome suspension. Applicator devices can include at least one of: a roller, a brush, a sponge, a swab, a tube, a lipstick. The taste of the at least one of a mast cell stabilizer and an antihistamine can be masked by flavors.Type: ApplicationFiled: February 2, 2012Publication date: January 31, 2013Inventors: Ziv Harish, Isaac Rubinstein, Russ Weinzimmer, Ehud Arbit
-
Patent number: 8263790Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: June 1, 2011Date of Patent: September 11, 2012Assignees: Children's Hospital Medical Center, Girindus America, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
-
Patent number: 8178702Abstract: A composition comprising compound of formula I, a process for preparing the composition comprising compound of formula I, methods of authentication for an article comprising compound of formula I or compound of formula II, authentication technology for polymer based articles comprising compound of formula I or formula II, methods of facilitating such authentication and method of making articles capable of authentication.Type: GrantFiled: May 16, 2008Date of Patent: May 15, 2012Assignee: Sabic Innovative Plastics IP B.V.Inventors: Yogendrasinh Chauhan, Mahesh Chaudhari, Adil Dhalla, Sriramakrishna Maruvada, Shantaram Naik, Vandita Pai-Paranjape, Philippe Schottland, Ganapati Shankarling, Kiran Puthamane, Meerakani Sait
-
Publication number: 20120058049Abstract: Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula (I), or formula (II); wherein X is OH, C1-C6 alkoxyl, 18F, or 19F; Y and Z are independently selected from a C1-C6 alkyl, CpC6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H, X is not OH.Type: ApplicationFiled: January 29, 2010Publication date: March 8, 2012Inventors: David R. Elmaleh, Timothy Shoup
-
Patent number: 8088935Abstract: Compounds and methods for the treatment of asthma are disclosed. The methods involve mast cell stabilization together with selective inhibition of iNOS. The compounds are combinations of a mast cell inhibiting moiety and an inhibitor of iNOS.Type: GrantFiled: December 23, 2004Date of Patent: January 3, 2012Assignee: Ironwood Pharmaceuticals, Inc.Inventors: James Pearson, John J. Talley, Mark G. Currie
-
Publication number: 20110144195Abstract: Two distinct methods are disclosed and claimed for synthesizing glyceollin I plus glyceollin II as a mixture and as their pure forms. Stereochemical isomers and various synthetic intermediates are also synthesized and claimed for their novel compositions of matter. All compounds and their mixtures are claimed for use in formulations that are useful to treat or prevent cancer, or that have utility as selective estrogen receptor modulators, such formulations including enhanced or medical foods, dietary supplements and ethical pharmaceutical agents.Type: ApplicationFiled: March 3, 2009Publication date: June 16, 2011Inventors: Paul W. Erhardt, Rahul Khupse, Jeffrerey G. Sarver, Thomas E. Cleveland, Stephen M. Boue, Thomas E. Wiese, Matthew E. Burow, John A. McClachlan
-
Patent number: 7960573Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: May 4, 2009Date of Patent: June 14, 2011Assignees: Children's Hospital Medical Center, Girindus America, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
-
Publication number: 20110112183Abstract: The invention provides oligomer-bis-chromonyl compound conjugates. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: ApplicationFiled: April 23, 2009Publication date: May 12, 2011Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
-
Patent number: 7932405Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.Type: GrantFiled: November 10, 2008Date of Patent: April 26, 2011Assignee: Aryx Therapeutics, Inc.Inventors: Pascal Druzgala, Cyrus Becker
-
Patent number: 7851640Abstract: Various chromanone, flavanone and abyssinone compounds as can be prepared enantioselectively using a chiral thiourea catalyst.Type: GrantFiled: March 2, 2009Date of Patent: December 14, 2010Assignee: Northwestern UniversityInventors: Karl Scheidt, Margaret Marie Biddle
-
Patent number: 7816544Abstract: The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.Type: GrantFiled: March 23, 2005Date of Patent: October 19, 2010Assignee: Trustees of Boston UniversityInventors: Guilford Jones, II, Baudouin Gerard, John A. Porco, Jr.
-
Patent number: 7795300Abstract: The present invention relates to an external preparation for skin comprising a compound, such as centaureidin(5,7-dihydroxy-3,6-dimethoxy-2-(5-hydroxy-4-methoxyphenyl)-4H-1-benzopyran-4-one); 5,7-dihydroxy-3,6,8-trimethoxy-2-(3,4,5-trihydroxyphenyl)-4H-1-benzopyran-4-one; 3,5-diethoxy-6,7-dimethoxy-2-(5-ethoxy-4-methoxyphenyl)-4H-1-benzopyran-4-one; and 5,6-dihydroxy-3,7-dimethoxy-2-(5-hydroxy-2,4-dimethoxyphenyl)-4H-1-benzopyran-4-one; and/or salt thereof and 4-n-butyl resorcinol and/or a salt thereof. The present invention provides an external preparation for skin having a function as a substantial lightening cosmetic that exerts whitening action of inhibiting excessive melanin production and keeping natural-looking whiteness.Type: GrantFiled: December 14, 2004Date of Patent: September 14, 2010Assignees: Kuraray Co., Ltd., Pola Chemical Industries Inc.Inventors: Akihiro Tada, Akiko Kanamaru
-
Publication number: 20100094026Abstract: The present invention provides a method of screening for a compound useful for treatment of an allergic disease by identifying a molecule targeted by Intal upon exertion of its efficacy as an anti-allergic agent (hereinafter referred as a target) and using the target, as well as a new type of anti-allergic agent comprising a compound obtainable by the screening as an active ingredient for treatment of an allergic disease.Type: ApplicationFiled: August 11, 2006Publication date: April 15, 2010Applicant: REVERSE PROTEOMICS RESEARCH INSTITUTE CO., LTD.Inventors: Akito Tanaka, Akinobu Nakanishi, Masayuki Haramura, Mikio Takeuchi
-
Publication number: 20090324540Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: ApplicationFiled: June 10, 2009Publication date: December 31, 2009Applicant: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
-
Patent number: 7638514Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtType: GrantFiled: August 25, 2004Date of Patent: December 29, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
-
Publication number: 20090264664Abstract: Mast cell degranulation inhibitors having a carboxyl group have not been developed as external preparations due to the low transdermal permeability thereof. By formulating external preparations thereof, side effects on the internal organs by oral administration can be avoided. Some of the mast cell degranulation inhibitors show drastically inferior photostability, which is also one cause of suppressed development of the drug as an external preparation. The present invention aims at improving the transdermal permeability and photostability of mast cell degranulation inhibitors by forming a salt of the mast cell degranulation inhibitor with an organic amine. Consequently, an external preparation of a mast cell degranulation inhibitor can be provided and the photostability of the mast cell degranulation inhibitor itself, and a preparation containing same can be improved.Type: ApplicationFiled: October 20, 2006Publication date: October 22, 2009Applicant: MEDRX CO., LTD.Inventors: Mitsuru Endo, Hidetoshi Hamamoto, Keiko Yamasaki, Sueko Matsumura
-
Publication number: 20090239916Abstract: The present invention provides a pharmaceutical composition comprising as an active ingredient a compound that specifically binds to MFP-2 or a functional fragment thereof and a screening method for the compound; the compound and a pharmaceutical composition comprising the same are highly useful as anti-inflammatory agents and anti-allergic agents.Type: ApplicationFiled: May 26, 2005Publication date: September 24, 2009Applicant: Reverse Proteomics Research Institute Co., LtdInventors: Akito Tanaka, Akira Yamazaki, Akinobu Nakanishi, Mikio Takeuchi, Masayuki Haramura
-
Publication number: 20090234023Abstract: The present invention relates to substituted hydroxyacetophenone derivatives having antiproliferative and antimicrobial properties, to pharmaceutical compositions containing them, as well as to a method of preparing them. Moreover, the hydroxyacetophenone derivatives according to the invention can serve as organic intermediates for the preparation of biologically active compounds.Type: ApplicationFiled: July 6, 2005Publication date: September 17, 2009Applicant: Riemser Arzneimittel AGInventors: Jose Agustin Quincoces Suarez, Klaus Peseke, Ernesto Estrada Roger
-
Publication number: 20090215881Abstract: Cosmetic and therapeutic, in particular dermatological bioprecursors have the formula [A]n—PP—[B]m wherein PP is a polyphenol radical in which each hydroxyl function is protected by a group A or a group B, A is a saturated or unsaturated, substituted or unsubstituted alkyl radical having 1 to 20 carbon atoms which is bonded to the polyphenol, n is an integer not less than 1, and B is a precursor of a biologically active molecule, which is also bonded to the polyphenol, and m is an integer also not less than 1.Type: ApplicationFiled: June 16, 2006Publication date: August 27, 2009Applicants: CHANEL PARFUMS BEAUTEInventors: Sabine Delaire, Adrien Adao, Jean-Roger Desmurs, Mirjana Gelo-Pujic, Laurent Saint-Jalmes, Tarek Kassem
-
Patent number: 7528267Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: August 1, 2005Date of Patent: May 5, 2009Assignees: Girindus America, Inc., Children's Hospital Medical CenterInventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
-
Patent number: 7524883Abstract: The present invention provides compounds having formula (1): wherein R1-R6, A, J, D, E, G, Q, w, x, y, and z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of cancer and/or inflammatory disorders, and more generally as proteasome inhibitors.Type: GrantFiled: January 8, 2003Date of Patent: April 28, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Sergei Agoulnik, Kozo Akasaka, Frank Fang, Jean-Christophe Harmange, Lynn Hawkins, Yimin Jiang, Charles Johannes, Xiang-Yi Li, Pamela McGuiness, Erin A. Murphy, Shawn Schiller, Mary Vermeulen, Jiayi Wu
-
Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
-
Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
-
Publication number: 20080177093Abstract: The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.Type: ApplicationFiled: March 23, 2005Publication date: July 24, 2008Inventors: Guilford Jones ll, Baudouin Gerard, John A. Porco Jr
-
Patent number: 7368434Abstract: The present invention provides novel antidipsotropic compounds. The invention further provides methods of inhibiting ALDH-2 using the compounds described herein. Methods for modulating alcohol consumption, alcohol dependence and/or alcohol abuse by administering the compounds of the invention to an individual are also provided. The present invention further provides a rationale for designing additional novel antidipsotropic compounds.Type: GrantFiled: June 27, 2003Date of Patent: May 6, 2008Assignee: The Endowment for Research in Human Biology, Inc.Inventors: Wing Ming Keung, Bert L. Vallee, Guangyao Gao
-
Publication number: 20080039640Abstract: A process for the preparation of a compound of formula (I) or a salt thereof wherein R is an amino, nitro or —NHCOR1 group, wherein R1 is C1-C6 alkyl or phenyl optionally substituted by a —O—(CH2)n-phenyl group, wherein n is an integer of 1 to 6; comprising reacting a compound of formula (II) or a salt thereof, both as the individual isomer and as an isomeric mixture, wherein R is as defined above; with a dehydrating agent, if necessary in the presence of an organic solvent, and optionally in the presence of a basic agent; and, if desired, converting a compound of formula (I) to another compound of formula (I) or a salt thereof.Type: ApplicationFiled: August 8, 2007Publication date: February 14, 2008Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Lino COLOMBO, Pietro ALLEGRINI, Alessandra AMOROSI, Gabriele RAZZETTI, Roberto ROSSI
-
Publication number: 20080021095Abstract: The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of XIAP family proteins. In particular, the present invention provides embelin and other XIAP inhibitors and methods of using these compounds as antagonists of the anti-apoptotic effects of XIAP family member proteins. The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases).Type: ApplicationFiled: March 22, 2005Publication date: January 24, 2008Inventors: Jianyong Chen, Zaneta Nikolovska-Coleska, Dajun Yang, Shaomeng Wang, Haiying Sun, Liang Xu, Zengjian Hu
-
Publication number: 20070238712Abstract: 19-nor-vitamin D analogs having an additional heterocyclic ring connecting the 3?-oxygen and carbon-2 or the 1?-oxygen and carbon-2 of the A-ring of the analog, and pharmaceutical uses therefore, are described. These compounds exhibit significant activity in mobilization of bone, making them therapeutic agents for the treatment or prophylaxis of osteoporosis, osteomalacia, osteopenia, renal osteodystrophy and hypoparathyroidism.Type: ApplicationFiled: April 6, 2007Publication date: October 11, 2007Inventors: Hector F. DeLuca, Rafal R. Sicinski, Agnieszka Glebocka, Lori A. Plum, Margaret Clagett-Dame
-
Patent number: 7141601Abstract: The present invention relates to a dendrite elongation inhibitor for melanocytes consisting of a compound represented by the following general formula (1): and/or a salt thereof, wherein R1, R2, and R3 each independently represent a C1-4 alkyl group or hydrogen atom, and a skin preparation for external use comprising the dendrite elongation inhibitor for melanocytes as an active ingredient.Type: GrantFiled: November 28, 2003Date of Patent: November 28, 2006Assignee: Pola Chemiocal Industries Inc.Inventors: Akihiro Tada, Akiko Kanamaru, Yuko Saeki
-
Patent number: 7094914Abstract: A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2): wherein R1, R2 and the wavy line have the same meanings as the above, and one of X2 and X3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3): in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5): wherein R1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.Type: GrantFiled: February 27, 2003Date of Patent: August 22, 2006Assignees: Sumitomo Chemical Company, Limited, Ono Pharmaceutical Co., Ltd.Inventors: Hiroaki Hibino, Susumu Ohtsuka, Yasunobu Miyamoto, Tomoyasu Yoshida, Itsuo Okumoto
-
Patent number: 6818668Abstract: A compound is provided for increasing the concentration of a parent isoflavone in a subject in vivo. The parent isoflavone has a skeletal structure including a 5 position and a 7 position, a 5 alkyl group, and a 7-hydroxy group with a 7-hydroxy oxygen appended to the 7 position and a 7-hydroxy hydrogen appended to the 7-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent isoflavone, with a 5 position and a 7 position corresponding to the 5 and 7 positions respectively of the parent isoflavone. An alkyl group is appended to the 5 position. A promoiety is appended to the 7-hydroxy oxygen of the substrate as a substitute for the 7-hydroxy hydrogen of the parent isoflavone, the promoiety and the 7-hydroxy oxygen establishing an alkylcarbonate ester. A related method also is provided.Type: GrantFiled: April 12, 2002Date of Patent: November 16, 2004Assignee: Biotest Laboratories, LLCInventor: William J. Roberts
-
Patent number: 6645997Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: September 24, 2001Date of Patent: November 11, 2003Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
-
Patent number: 6630506Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g.Type: GrantFiled: April 21, 2000Date of Patent: October 7, 2003Assignee: Bristol-Myers Squibb Co.Inventors: Sundeep Dugar, Steven V. O'Neil
-
Patent number: 6566508Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: March 11, 2002Date of Patent: May 20, 2003Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski
-
Patent number: 6552054Abstract: The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.Type: GrantFiled: March 1, 2002Date of Patent: April 22, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Masahiro Kawase, Akira Mori
-
Patent number: 6541613Abstract: Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hyrolyzable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs.Type: GrantFiled: December 15, 2000Date of Patent: April 1, 2003Assignee: Uyrex CorporationInventors: Sheldon S. Hendler, Jan Zielinski
-
Publication number: 20020128494Abstract: The invention relates to new flavone derivaties which have at least one N-disubstituted carbamoyloxy unit (OOCNR6(R7))coupled directly to one or both aromatic rings of the flavone molecule.Type: ApplicationFiled: September 21, 2001Publication date: September 12, 2002Inventors: Ildiko B. Mihokne, Gyorgy Toth, Sandor Molnar, Tivadar Tamas, Gyorgy Sulyok, Eva K. Mudrane
-
Patent number: 6372895Abstract: Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when cleaved by target enzymes. Preferred compounds include sugar and peptide derivatives of umbelliferone derivatives bearing a heterocyclic five membered ring at the 3-position. These compounds can be used for rapidly detecting food pathogens and for determining sterilization effectiveness. The compounds may also be used in a form bounded to a polymeric support or to a biomolecule or macromolecule.Type: GrantFiled: July 7, 2000Date of Patent: April 16, 2002Assignee: 3M Innovative Properties CompanyInventors: James Gregory Bentsen, Christopher Allen Mickelson, Orlin Bruce Knudson, Kevin Michael Lewandowski