The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/151)
  • Patent number: 9394268
    Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogs. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: July 19, 2016
    Assignee: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Patent number: 9371305
    Abstract: The present invention discloses deuterated benzopyran compounds having structure features as shown in Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or prodrug molecules thereof. With excellent anti-inflammatory and analgesic effects and the capability to inhibit growth of tumor cells, such compounds are novel COX-2 selective inhibitors. The compounds and pharmaceutically acceptable salts thereof disclosed by the present application can be applied in preparing anti-inflammatory and analgesic drugs and drugs for treating or preventing tumors.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: June 21, 2016
    Assignee: Guangzhou Institutes of Biomedicine And Health, Chinese Academy of Sciences
    Inventors: Yanmei Zhang, John Jeffrey Talley, Mark G. Obukowicz, Zhengchao Tu, Micky Tortorella, Yican Wang, Jianqi Liu, Yan Chen, Xiaorong Liu, Xin Lu
  • Publication number: 20150141252
    Abstract: A method of screening for a plant defense activator, which enhances an immune response of a plant, from at least one candidate substance includes: contacting a plant cell in which a jasmonic acid-dependent defense pathway and a salicylic acid-dependent defense pathway of a plant defense system are capable of working independently from each other, with a candidate substance; contacting the plant cell with a trigger material that induces an immune response; and assaying the plant cell after contacting with the trigger material based on an index representing an immune response, to select a target substance that enhances an immune response of the plant. A method of enhancing an immune response of a plant includes use of a specific compound, and a plant immune response enhancer includes the specific compound.
    Type: Application
    Filed: August 10, 2011
    Publication date: May 21, 2015
    Applicant: Tokyo University of Science Foundation
    Inventors: Kazuyuki Kuchitsu, Takamitsu Kurusu
  • Publication number: 20150133659
    Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogues. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 14, 2015
    Applicant: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Publication number: 20150111888
    Abstract: The present invention provides a small compound targeting at TACC3. The present invention further provides a drug, particularly, an anticancer agent, comprising the small compound targeting at TACC3. A compound represented by the general formula (I) or a pharmaceutically acceptable salt, solvate, or ester derivative thereof binds to TACC3 and inhibits cell growth. Thus, these compounds can be used as drugs, particularly, anticancer agents.
    Type: Application
    Filed: April 30, 2013
    Publication date: April 23, 2015
    Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
  • Publication number: 20150045358
    Abstract: A pharmaceutical composition for treating disorders associated with insulin resistance is disclosed, and the composition comprises at least one inhibitor which is an effective agent to suppress endothelin-1-stimulated resistin gene expression through decreasing the endothelin-1-stimulated phosphorylation of proteins downstream of endothelin type A receptor, wherein the downstream signaling molecules comprise ERK1/2, JNKs, AKT, and STAT3 proteins, and wherein the inhibitor is selected from at least one antagonist of the endothelin type A receptor or downstream signaling proteins.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 12, 2015
    Inventors: Yung-hsi KAO, Ya-chu Tang, Hsin-huei Chang, Hui-chen Ku
  • Publication number: 20140364427
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: December 14, 2012
    Publication date: December 11, 2014
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Andiliy G. Lai
  • Publication number: 20140322278
    Abstract: Compositions and methods are provided for modulating the physiological activation of tissue transglutaminase (TG2); which methods can include inhibiting the activation of TG2 associated with enteric inflammatory disorders, which disorders may include celiac disease, irritable bowel syndrome, Crohn's Disease, dermatitis herpetiformis, and the like. In other embodiments of the invention, methods are provided for reducing undesirable paracellular transport in enteric tissues, in particular the paracellular transport of molecules greater than about 500 mw, e.g. peptides, including without limitation immunogenic gluten peptides.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 30, 2014
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Thomas DiRaimondo, Xi Jin, Cornelius Kloeck, Chaitan Khosla
  • Patent number: 8865052
    Abstract: The TPU of this invention contains unsaturation in its polymeric backbone. The unsaturation can be present in the soft segment or in the hard segment or in both the soft and hard segments of the TPU. The TPU can be molded like a thermoplastic, and can be subsequently crosslinked by exposure to electron beam irradiation into thermoset articles having excellent chemical resistance, dimensional stability, set properties, heat resistance, oxidative resistance, and creep resistance. In one embodiment, the TPUs of this invention are the reaction product (1) a hydroxyl terminated intermediate, (2) a polyisocyanate, (3) a saturated glycol chain extender, and (4) a glycol chain extender containing carbon-carbon double bonds, such as the allyl moieties present in trimethylolpropane monoallyl ether.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: October 21, 2014
    Assignee: Lubrizol Advanced Materials, Inc.
    Inventors: Umit G. Makal, Louis J. Brandewiede, George H. Loeber
  • Publication number: 20140296232
    Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicants: Massachusetts General Hospital, The Broad Institute, Inc.
    Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
  • Publication number: 20140275068
    Abstract: The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1. The compounds are useful for the treatment or prevention of a range of conditions including, e.g., migraine, epilepsy, non-epileptic seizures, brain injury, and cardiovascular disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Proximagen Limited
    Inventors: Edward Savory, Daniel Hill, Oldrich Kocian
  • Publication number: 20140080827
    Abstract: 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: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20130345420
    Abstract: The invention is the discovery of the use of the class of compounds represented by Formula I, as selective inhibitors of excitatory amino acid transporter (EAAT) subtype 1 (EAAT1) and its rodent ortholog L-glutamate/L-aspartate transporter (GLAST) for the study of function and distribution of EAAT1/GLAST in the central nervous system and studies of the physiological and pathological functions of the EAAT1/GLAST subtype in native tissues, cultured neurons, and/or animal models for CNS disorders.
    Type: Application
    Filed: September 19, 2011
    Publication date: December 26, 2013
    Inventors: Lennart Bunch, Anders Asbjørn Jensen
  • Patent number: 8546376
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: October 1, 2013
    Assignee: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Publication number: 20130158261
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: TaiMed Biologics, Inc.
    Inventor: TaiMed Biologics, Inc.
  • Publication number: 20130116232
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: June 8, 2011
    Publication date: May 9, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
  • Publication number: 20130116247
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 9, 2013
    Applicant: MANNKIND CORPORATION
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Patent number: 8399460
    Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: March 19, 2013
    Assignee: Astrazeneca AB
    Inventors: Bernard Chistrophe Barlaam, Sebastien Louis Degorce, Christine Marie Paul Lambert-Van Der Brempt, Remy Robert Morgentin, Patrick Ple
  • Patent number: 8394794
    Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: March 12, 2013
    Assignee: Regents of The University of Minnesota
    Inventors: Chengguo Xing, Jignesh Doshi
  • Publication number: 20130040947
    Abstract: Compounds and methods related to the activation of the TrkB receptor are provided. The methods include administering a 7,8-di-hydroxyflavone derivative with modified flavone or heterocyclic ring to a subject in need thereof. Methods and compounds for the treatment of disorders including neurologic disorders, neuropsychiatric disorders, and metabolic disorders (e.g., obesity) are provided.
    Type: Application
    Filed: June 8, 2011
    Publication date: February 14, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Publication number: 20130035323
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
  • Patent number: 8273905
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: September 25, 2012
    Assignee: Abbott Products GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Publication number: 20120238541
    Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 20, 2012
    Applicant: Almac Discovery Limited
    Inventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
  • Publication number: 20120238566
    Abstract: Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8.
    Type: Application
    Filed: April 27, 2010
    Publication date: September 20, 2012
    Inventors: Chengyu Jiang, Shuan Rao, Haolin Liu, Feng Guo, Hongliang Wang, Yang Sun, Chenggang Li
  • Patent number: 8242115
    Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 14, 2012
    Assignee: Luitpold Pharmaceuticals, Inc.
    Inventors: James Halbrook, Edward A. Kesicki, Laurence E. Burgess, Stephen T. Schlachter, Charles T. Eary, Justin G. Schiro, Hongmei Huang, Michael Evans, Yongxin Han
  • Publication number: 20120059001
    Abstract: 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: Application
    Filed: November 9, 2011
    Publication date: March 8, 2012
    Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SA
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20120035361
    Abstract: The invention is the discovery of the use of the class of compounds represented by Formula I, as selective inhibitors of excitatory amino acid transporter (EAAT) subtype 1 (EAAT1) and its rodent ortholog L-glutamate/L-aspartate transporter (GLAST) for the study of function and distribution of EAAT1/GLAST in the central nervous system and studies of the physiological and pathological functions of the EAAT1/GLAST subtype in native tissues, cultured neurons, and/or animal models for CNS disorders.
    Type: Application
    Filed: September 19, 2011
    Publication date: February 9, 2012
    Inventors: Lennart Bunch, Anders Asbjørn Jensen
  • Publication number: 20120022062
    Abstract: The present invention relates to flavanoid compounds of general formula (X1) wherein: R1 is selected from a group consisting of morpholinyl, N-methyl piperizinyl, piperidinyl and N,N?-dimethylamino groups, and n ranges from 3 to 6, and process for preparation thereof. The present invention relates to the demonstration of anti Helicobacter pylori activity and gastric antisecretory activity of semisynthetically designed flavonoid compounds, to be used for the prevention and treatment of gastroduodenal disorders in general and peptic ulcer diseases in particular. The present invention also relates to a hetero-dimeric bi-functional molecule that can be used as monotherapy substituting/replacing/overcoming currently used triple/quadruple therapy, thereby implicating/anticipating/envisaging its commercial applicability.
    Type: Application
    Filed: February 26, 2010
    Publication date: January 26, 2012
    Inventors: Pratap Kumar Dab, Suchandra Goswami, Annalaskhmi Chinniah, Janaswamy Madusudana Rao, Suresh Babu Katragadda
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20110207729
    Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia, and the like, based on the serotonin 5-HT5A receptor modulating action. It was confirmed that a bicyclic acylguanidine derivative which has a characteristic structure that guanidine is bonded to one ring of a bicyclic structure such as chromene and dihydronaphthalene through a carbonyl group and a cyclic group is bonded on the other ring, has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based on this mechanism. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder.
    Type: Application
    Filed: August 7, 2008
    Publication date: August 25, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Isao Kinoyama, Satoshi Miyamoto, Takehiro Miyazaki, Yohei Koganemaru, Yuichiro Kawamoto, Nobuyuki Shiraishi, Hiroaki Hoshii, Akio Kuroda, Mayako Yamazaki, Minoru Yasuda, Hiroaki Mizuno
  • Publication number: 20110118257
    Abstract: 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: Application
    Filed: November 3, 2010
    Publication date: May 19, 2011
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Publication number: 20110098271
    Abstract: The invention concerns chromenone derivatives of Formula I or a pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, R6, R7, R8, n and R9 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Application
    Filed: October 22, 2010
    Publication date: April 28, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Bernard Christophe BARLAAM, Sebastien Louis DEGORCE, Christine Marie Paul LAMBERT-VAN DER BREMPT, Remy Robert MORGENTIN, Patrick PLE
  • Publication number: 20110021522
    Abstract: The present invention provides compounds as activators of procaspases 3, 6 and/or 7 and related derivatives, pharmaceutical compositions thereof, methods for their use, and methods for preparing these compounds. In one aspect, the compounds are useful for treating cancers and neoplastic diseases.
    Type: Application
    Filed: January 9, 2009
    Publication date: January 27, 2011
    Applicant: The Regents of the University of California
    Inventors: Jim Wells, Adam R. Renslo, Dennis Wolan, Julie Zorn
  • Patent number: 7872004
    Abstract: The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: January 18, 2011
    Assignee: Japan Tobacco Inc.
    Inventors: Motohide Satoh, Hisateru Aramaki, Masaki Yamashita, Masafumi Inoue, Hiroshi Kawakami, Hisashi Shinkai, Hiroshi Nakamura, Yuji Matsuzaki, Shuichi Wamaki
  • Patent number: 7829557
    Abstract: The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.
    Type: Grant
    Filed: August 28, 2006
    Date of Patent: November 9, 2010
    Assignee: The Ohio State University Research Foundation
    Inventors: Robert W. Brueggemeier, Young-Woo Kim
  • Patent number: 7812019
    Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
    Type: Grant
    Filed: November 22, 2005
    Date of Patent: October 12, 2010
    Assignee: Abbott Laboratories
    Inventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
  • Publication number: 20100222338
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: May 13, 2010
    Publication date: September 2, 2010
    Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
  • Publication number: 20100197686
    Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
    Type: Application
    Filed: March 21, 2008
    Publication date: August 5, 2010
    Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventors: Chengguo Xing, Jignesh Doshi
  • Publication number: 20100144729
    Abstract: A compound of formula (I) wherein R1, R2, R3 and R4 are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Application
    Filed: January 31, 2008
    Publication date: June 10, 2010
    Inventors: Rolf Baenteli, Nigel Graham Cooke, Frederic Zecri, Alexander Baxter Smith
  • Publication number: 20100130736
    Abstract: Drug discovery is a complex undertaking facing many challenges, not the least of which is a high attrition rate as many promising candidates prove ineffective or toxic in the clinic owing to a poor understanding of the diseases, and thus the biological systems, they target. Therefore, it is broadly agreed that to increase the productivity of drug discovery one needs a far deeper understanding of the molecular mechanisms of diseases, taking into account the full biological context of the drug target and moving beyond individual genes and proteins. The present methods rely on the use of label-free cellular assays, particularly the DMR index, to systematically display the mode of actions, the toxicity, and the target(s) and pathway(s) of any molecules.
    Type: Application
    Filed: November 23, 2009
    Publication date: May 27, 2010
    Inventors: Ye Fang, Ann M. Ferrie, Joydeep Lahiri, Elizabeth Tran
  • Patent number: 7714150
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: May 11, 2010
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Patent number: 7662977
    Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: February 16, 2010
    Assignee: Semafore Pharmaceuticals, Inc.
    Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
  • Publication number: 20090312317
    Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.
    Type: Application
    Filed: June 10, 2009
    Publication date: December 17, 2009
    Applicant: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Jang-Yang Chang, Ching-Chuan Kuo, Yu-Sheng Chao
  • Publication number: 20090215768
    Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: October 1, 2008
    Publication date: August 27, 2009
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Gwo-Jaw Wang, Mai-Ling Ho, Je-Ken Chang, Yin-Chih Fu
  • Publication number: 20090215767
    Abstract: An isoflavone derivative is provided. The isoxazole derivative has following formula: wherein R1 and R2, independently, include C1-C12 alkyl optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy, and R3 includes hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis including an isoflavone derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: September 30, 2008
    Publication date: August 27, 2009
    Inventors: Cherng-Chyi TZENG, Yeh-Long Chen, Gwo-Jaw Wang, Mei-Ling Ho, Je-Ken Chang, Yin-Chih Fu
  • Publication number: 20090209533
    Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.
    Type: Application
    Filed: February 13, 2009
    Publication date: August 20, 2009
    Inventors: Jeff Zablocki, Matthew Abelman, Michael Organ, Yaroslav Bilokin, Elfatih Elzein, Tetsuya Kobayashi, Rao Kalla, Thao Perry, Xiaofen Li, Robert Jiang, Ivan Diamond, Lina Yao, Peidong Fan, Maria Pia Arolfo, Zhan Jiang, Wing Ming Keung, Guoxin Tao
  • Publication number: 20090203685
    Abstract: The present invention is directed to molecules deriving from a 3-aryl-coumarine or 3-aryl-quinolin-2-one and having potent anti-proliferative and/or cytotoxic activity, especially against tumoral cells. The present invention also concerns the uses of these molecules in therapeutic application, for the treatment of different cancers. The invention also discloses the use of said compound for the manufacture of a medicament for treating cancer. The invention also concerns a process for inhibiting cell proliferation comprising contacting said cells with a compound of the invention.
    Type: Application
    Filed: May 22, 2007
    Publication date: August 13, 2009
    Applicant: EOS (ETHICAL ONCOLOGY SCIENCE) S.P.A.
    Inventors: Matthieu Schapira, Cyrille Lamigeon, Mathieu Gutmann, Audrey Barthelaix, Nicolas Hugo, Pierre Colas
  • Publication number: 20090203686
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Application
    Filed: February 27, 2009
    Publication date: August 13, 2009
    Applicant: Solvay Pharmaceuticals GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Patent number: 7572791
    Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.
    Type: Grant
    Filed: January 24, 2008
    Date of Patent: August 11, 2009
    Assignee: AstraZeneca AB
    Inventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
  • Publication number: 20090048224
    Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: September 5, 2008
    Publication date: February 19, 2009
    Applicants: Amgen, Inc., Array BioPharma, Inc.
    Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak