Acyclic -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Lactone Ring Patents (Class 549/287)
  • Patent number: 9814696
    Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2-amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: November 14, 2017
    Assignees: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6), UNIVERSITE DE LIEGE
    Inventors: Michele Reboud-Ravaux, Chahrazade Yerroum-El Amri, Xiao Tan, Lixian Qin, Maurice Pagano, Alain Hovnanian, Laetitia Furio, Bernard Pirotte
  • Patent number: 9701667
    Abstract: There are provided fluorescent labelling agents comprising a dimaleimide core connected to a fluorophore, processes for preparation thereof, and uses thereof for labelling and/or detection of specific protein targets. Fluorescent labelling agents comprising a compound having the structure of Formula I, and salts thereof, are described.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: July 11, 2017
    Assignee: UNIVERSITY OF OTTAWA
    Inventors: Jeffrey Keillor, Yingche Chen
  • Patent number: 9006466
    Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: April 14, 2015
    Assignees: Universite Pierre et Marie Curie (Paris 6), Universite de Liege
    Inventors: Michele Reboud-Ravaux, Chahrazade Yerroum-El Amri, Xiao Tan, Lixian Qin, Maurice Pagano, Alain Hovnanian, Laetitia Furio, Bernard Pirotte
  • Publication number: 20140371272
    Abstract: The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula (I).
    Type: Application
    Filed: January 18, 2013
    Publication date: December 18, 2014
    Inventors: Venkatram R. Mereddy, Lester R. Drewes, Mohammed Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
  • Publication number: 20140242606
    Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 28, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
  • Patent number: 8815940
    Abstract: The present invention relates to certain coumarin/chalcone compounds or a pharmaceutically acceptable salt thereof. The present invention particularly relates to the coumarin/chalcone compounds as anticancer agents useful for the treatment of cancer. The present invention also relates to the process of preparation of the said compounds.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: August 26, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Koneni Venkata Sashidhara, Abdhesh Kumar, Manoj Kumar, Jayanta Sarkar, Sudhir Kumar Sinha
  • Publication number: 20140221673
    Abstract: A resist composition including a base component (A) which exhibits changed solubility in a developing solution under action of acid and an acid-generator component (B) which generates acid upon exposure, the base component (A) containing a polymeric compound (A1) having a structural unit (a5) represented by general formula (a5-0) shown below (R1 represents a sulfur atom or an oxygen atom; R2 represents a single bond or a divalent linking group; and Y represents an aromatic hydrocarbon group or an aliphatic hydrocarbon group having a polycyclic group, provided that the aromatic hydrocarbon group or the aliphatic hydrocarbon may have a carbon atom or a hydrogen atom thereof substituted with a substituent.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 7, 2014
    Applicant: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Daichi Takaki, Daiju Shiono, Yoshiyuki Utsumi, Takaaki Kaiho
  • Publication number: 20140186878
    Abstract: Compounds are provided that are either fluorogenic or fluorophoric. Compositions and articles that include the compounds are also provided. Additionally, methods of detecting a microorganism using the compounds are provided. The compounds are fluorinated and can be used advantageously under acidic conditions.
    Type: Application
    Filed: March 5, 2012
    Publication date: July 3, 2014
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Stephen B. Roscoe, Shih-Hung Chou, Stephanie J. Moeller, Jesse D. Miller, Kurt J. Halverson, Jason W. Bjork
  • Publication number: 20140148480
    Abstract: A compound of formula (I-1) wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a —O—R12 group, wherein R12 is a C1-C7 alkyl, a group —CH2—O—CO—R5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group —O—R13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a —CH2— amine, R?1 represents a group chosen among hydrogen and —O—R14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.
    Type: Application
    Filed: January 15, 2014
    Publication date: May 29, 2014
    Applicant: UNIVERSITE PIERRE ET MARIE CURIE (PARIS 6)
    Inventors: Michele REBOUD-RAVAUX, Chahrazade YERROUM-EL AMRI, Xiao TAN, Lixian QIN, Maurice PAGANO, Alain HOVNANIAN, Laetitia FURIO, Bernard PIROTTE
  • Publication number: 20140114068
    Abstract: Disclosed are novel indanone derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The indanone derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: April 24, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Hae Soo Kim, Hee Chun Jeong, Pil Ho Kim, Soo Bong Han, Jin Soo Shin, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140051709
    Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.
    Type: Application
    Filed: August 16, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Sita REDDY, Lucio Comai, Nouri Neamati
  • Patent number: 8642788
    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: Grant
    Filed: January 9, 2009
    Date of Patent: February 4, 2014
    Assignee: The Regents of the University of California
    Inventors: Jim Wells, Adam R. Renslo, Dennis Wolan, Julie Zorn
  • Publication number: 20130245268
    Abstract: Disclosed herein is enantioselective synthetic method comprising reacting an enolisable C4-C50 organic anhydride with a second compound selected from the group consisting of an aldehyde, a ketone, an aldimine, a ketimine or a Michael Acceptor in the presence of a bifunctional organocatalyst. The reaction may find particular utility in the enantioselective synthesis of medicinally relevant heterocycles, such as dihydroisocoumarins and dihydroisoquinolinones.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 19, 2013
    Applicant: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD
    Inventors: Stephen J. Connon, Sean Tallon, Claudio Cornaggia, Francesco Manoni, Esther Torrente
  • Publication number: 20130210909
    Abstract: The present invention relates to certain coumarin/chalcone compounds or a pharmaceutically acceptable salt thereof. The present invention particularly relates to the coumarin/chalcone compounds as anticancer agents useful for the treatment of cancer. The present invention also relates to the process of preparation of the said compounds.
    Type: Application
    Filed: August 5, 2011
    Publication date: August 15, 2013
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Koneni Venkata Sashidhara, Abdhesh Kumar, Manoj Kumar, Jayanta Sarkar, Sudhir Kumar Sinha
  • Publication number: 20130157197
    Abstract: A resist composition comprising: a base component (A) that exhibits changed solubility in a developing solution by the action of acid; a photoreactive quencher (C); and an acid-generator component (B) that generates acid upon exposure, wherein the photoreactive quencher (C) contains a compound represented by general formula (c1) shown below. In the formula, R1 represents a hydrogen atom or a hydrocarbon group of 1 to 20 carbon atoms which may have a substituent; each of R2 and R3 independently represents a hydrogen atom or a hydrocarbon group of 1 to 20 carbon atoms which may have a substituent; at least two of R1 to R3 may be mutually bonded to form a ring; X represents an oxygen atom or a sulfur atom; n represents 0 or 1; and Z+ represents an organic cation.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 20, 2013
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventor: Tokyo Ohka Kogyo Co., Ltd
  • Publication number: 20130150254
    Abstract: The present invention provides systems and methods for production of activatable diazo-derivatives for use in labeling nucleotides. Labeling nucleotides is accomplished by contacting a stable hydrazide derivative of a detectable moiety with an activating polymer reagent which is used to directly label the nucleotide sample. Labeling occurs on the phosphate backbone of the nucleotide which does not perturb hybridization of the labeled nucleotide with its anti-sense strand. Since the method involves direct labeling, all types of nucleotides can be labeled without prior amplification or alteration.
    Type: Application
    Filed: December 6, 2011
    Publication date: June 13, 2013
    Inventors: John J. Naleway, Ying Jiang, Ryan Link-Cole
  • Publication number: 20130079394
    Abstract: This invention relates to novel coumarin derivatives, formulations comprising same, and to methods of making and using these compounds and formulations, which are useful as repellents against insects and/or pests. The compounds also prevent illness and disease caused by insect/pest-borne vectors, and provide safer, more effective alternatives to existing repellents. This invention also relates to novel methods for modeling and/or predicting the repellency of unknown compounds.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 28, 2013
    Applicants: CNRS (CENTRE NATIONAL RECHERCHE SCIENTIFIQUE), MERIAL LIMITED
    Inventors: Jean Delaveau, Pierre Nicolas Stebe, Nathalie Marchand-Geneste
  • Publication number: 20130040393
    Abstract: A fluorescent dye or fluorophore capable of forming complexes with mercury comprises 6,8-difluoro-7-hydroxy-2-oxo-2H-chromene-3-carboxylate amide, wherein the amide is formed by reacting the succinimidyl ester (Pacific Blue™) with an amino acid containing a thiol group, such as cysteine or glutathione. Mercury complexes of the fluorophore fluoresce when excited by a UV or violet laser diode, and the detected intensity can be calibrated to quantify the concentration of mercury in a sample reacted with the fluorophore.
    Type: Application
    Filed: August 9, 2012
    Publication date: February 14, 2013
    Applicant: LOS GATOS RESEARCH
    Inventors: Hong Jiao, Hannah Catterall
  • Publication number: 20120328661
    Abstract: The present invention relates to novel 2-oxo-2H-chromene-3-carboxamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: October 20, 2010
    Publication date: December 27, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Todd M. Heidelbaugh, John R. Cappiello, Phong X. Nguyen, Dario G. Gomez
  • Publication number: 20120121536
    Abstract: Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells.
    Type: Application
    Filed: March 24, 2011
    Publication date: May 17, 2012
    Applicant: OHIO UNIVERSITY
    Inventors: Xiaozhuo Chen, Stephen Bergmeier
  • Publication number: 20120107744
    Abstract: A resist composition containing a base component (A) which exhibits changed solubility in a developing solution under the action of acid, and an acid generator component (B) which generates acid upon exposure, wherein the acid generator component (B) includes an acid generator (B1) having a group represented by general formula (b1-1) shown below in the cation moiety.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 3, 2012
    Applicant: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Yoshiyuki Utsumi, Akiya Kawaue, Yoshitaka Komuro, Kenichiro Miyashita
  • Publication number: 20110217654
    Abstract: The invention pertains to a compound generating an acid of the formula I or II, for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes wherein X is CH2 or CO; Y is O, NR4, S, O(CO), O(CO)O, O(CO)NR4, OSO2, O(CS), or O(CS)NR4; R1 is for example C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, interrupted C2-C18alkyl, interrupted C3-C30cycloalkyl, interrupted C3-C30cycloalkyl-C1-C18alkyl, interrupted C4-C30cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R1 is NR12R13; R2 and R3 are for example C3-C30cycloalkylene, C3-C30cycloalkyl-C1-C18alkylene, C1-C18alkylene, C1-C10haloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R4 is for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18al
    Type: Application
    Filed: February 16, 2011
    Publication date: September 8, 2011
    Applicant: BASF SE
    Inventors: Hitoshi Yamato, Toshikage Asakura, Akira Matsumoto, Keita Tanaka, Yuichi Nishimae
  • Publication number: 20110172442
    Abstract: The amino acid derivative of the present invention provides a novel compound that shows excellent analgesic action. The amino acid derivative of the present invention is a novel compound that shows excellent analgesic action to not only a model animal for nociceptive pains but also a model animal for neuropathic pains, so that the amino acid derivative is very useful as a drug for treating various pain diseases.
    Type: Application
    Filed: September 17, 2009
    Publication date: July 14, 2011
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiro Ookubo, Ko Nakamura, Hiroyoshi Nanba, Hiroyuki Yoshida, Yoshitaka Nakazawa
  • Publication number: 20110142717
    Abstract: The present invention generally relates to luminescent and/or optically absorbing compositions and/or precursors to those compositions, including solid films incorporating these compositions/precursors, exhibiting increased luminescent lifetimes, quantum yields, enhanced stabilities and/or amplified emissions. The present invention also relates to sensors and methods for sensing analytes through luminescent and/or optically absorbing properties of these compositions and/or precursors. Examples of analytes detectable by the invention include electrophiles, alkylating agents, thionyl halides, and phosphate ester groups including phosphoryl halides, cyanides and thioates such as those found in certain chemical warfare agents. The present invention additionally relates to devices and methods for amplifying emissions, such as those produced using the above-described compositions and/or precursors, by incorporating the composition and/or precursor within a polymer having an energy migration pathway.
    Type: Application
    Filed: November 15, 2010
    Publication date: June 16, 2011
    Applicant: Massachusetts Institute of Technology
    Inventors: Timothy M. Swager, Tae-Hyun Kim, Shi-Wei Zhang
  • 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
  • Publication number: 20110015189
    Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1 may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.
    Type: Application
    Filed: July 20, 2009
    Publication date: January 20, 2011
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Bo CHEN, Zhi-Xian WANG, Yutao XUE, Lihong LIU, Hao CHEN
  • Publication number: 20100168225
    Abstract: Compounds of Formula 5 and prodrug compounds of Formula 5 wherein G1 is H or OH; G2 is H, R?, or CO2R?; G3, G4 and G5, are each independently selected from the group consisting of: H, R?, OH, OR?, F, Cl, Br, I, NH2, NHR?,NR?2, CN, SH, SR?, SO3H, SO3R?, SO2R?, OSO3R?, and NO2; and R? is a one to four carbon alkyl group are provided. Uses of these compounds and methods of medical treatment involving these compounds for the treatment of hepatitis C are also provided.
    Type: Application
    Filed: April 18, 2008
    Publication date: July 1, 2010
    Inventors: Francois Jean, Raymond Andersen
  • 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: 20090011454
    Abstract: The invention provides compounds of formulas I, II, and III, methods of making them, and methods of their use. The compounds of the invention can be used as fluorescent sensors, for example, to detect an amine-containing analyte in a biological sample. The compounds can be selective for one type of amine over others and the amount of fluorescence can be correlated with the concentration of the amine in the sample.
    Type: Application
    Filed: July 28, 2006
    Publication date: January 8, 2009
    Applicant: The Curators of the University of Missouri Office of Technology and Special Projects
    Inventors: Timothy Glass, Kevin Gillis, Kristen Secor
  • Patent number: 7405227
    Abstract: Methods of treating ovarian cancer, endometrium cancer, cervical cancer, pancreatic cancer, bladder cancer, eve cancer, central nervous system cancer, thyroid cancer and lung cancer are disclosed. Specifically disclosed are methods of treating ovarian adenocarcinoma that has migrated into the abdominal cavity, a transitional cell carcinoma of the bladder, an epithelioid carcinoma in a pancreatic duct, an adenocarcinoma in a pancreatic duct, an adenocarcinoma in the cervical epithelium. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: July 29, 2008
    Assignee: BiPAr Sciences, Inc.
    Inventors: Ernest Kun, Jerome Mendeleyev, Carol Basbaurn, Hassan Lemjabbar-Alaoui, Valeria Ossovskaya
  • Patent number: 7282575
    Abstract: A compound represented by the general formula (I) below: In the formula, A is as defined in the specification and B denotes where n is an integer of 1 to 4, and a process for producing the above compound includes a reaction between an activated ester and a t-butoxycarbonylaminoethylamine or an ?-amino acid derivative.
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: October 16, 2007
    Assignee: Credia Japan Co., Ltd.
    Inventors: Hisafumi Ikeda, Isao Saito, Fumihiko Kitagawa
  • Publication number: 20040014160
    Abstract: Coumarin derivative as a substrate for cytochrome P450 enzymes.
    Type: Application
    Filed: July 25, 2003
    Publication date: January 22, 2004
    Inventors: Jacqueline Carol Bloomer, Colin Andrew Leach
  • Publication number: 20030105340
    Abstract: The present invention provides a process from preparing isocoumarin-3-yl derivatives comprising reacting a homophthalic anhydride derivative with a carbonyl compound, wherein the carbonyl group is substituted with an acyl activating group, in the presence of a reaction medium comprising a solvent and a base. The invention also encompasses a process for the preparation of homophthalate esters useful in the preparation of homophthalic anhydride reactants as well as an integrated process wherein the twp reactions are carried out sequentially to afford the desired isocoumarin derivative.
    Type: Application
    Filed: July 2, 2002
    Publication date: June 5, 2003
    Inventors: William E. Bauta, William R. Cantrell, Dennis P. Lovett
  • Patent number: 6451846
    Abstract: The present invention relates to novel isocoumarin derivatves inhibiting angiogenesis, a method for preparation thereof and pharmaceutical compositions comprising the said derivatives as pharmaceutically active ingredients. More particularly, the present invention relates to novel isocoumarin derivatves represented by formula (1), especially 6,8-dihydroxy-4-acetyl-isocoumarin, a method for preparing 6,8-dihydroxy-4-acetyl-isocoumarin from fungi, and pharmaceutical compositions comprising the compounds and/or 6,8-dihydroxy-4-acetyl-isocoumarin as pharmaceutically active ingredients, which would be effective for the treatment of angiogenic diseases such as cancers, rheumatoid arthritis and diabetic retinopathy.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: September 17, 2002
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Jung Joon Lee, Hang-Sub Kim, Jeong-Hyung Lee, Young-Soo Hong, Yun Joo Park
  • Publication number: 20020127428
    Abstract: An organic light emitting display is provided which comprises as an emitting layer a fluorescent dye having at least one amine moiety substituted with two aryl groups. Also provided are new fluorescent compounds having N-aryl substituents which exhibit reduced pH sensitivity and enhanced stability to protonation.
    Type: Application
    Filed: March 6, 2001
    Publication date: September 12, 2002
    Applicant: International Business Machines Corporation
    Inventors: Sally Ann Swanson, Gregory Michael Wallraff
  • Publication number: 20020120155
    Abstract: An improved procedure for the purification of warfarin acid. Sodium, potassium and lithium warfarin salts and the corresponding clathrates are prepared in high, pharmacopeial grade purity and good yields from the pure warfarin acid and the respective metal salt bases in suitable media.
    Type: Application
    Filed: February 28, 2001
    Publication date: August 29, 2002
    Inventors: Sorin Bercovici, Yuval Evron, Osvaldo Fuxman, Mirela Jakoel, Sbar Sasson, Konstantin Ulanenko
  • Publication number: 20020086234
    Abstract: The present invention provides a novel ammonium salt of an organic acid. When the salt is used as a base additive for a chemically amplified resist, the environmental stability of the resist can be enhanced, and the T-top phenomenon can be effectively prevented. In addition, the line width change caused by acid diffusion can be prevented, and the E0 value of the resist can be decreased.
    Type: Application
    Filed: March 9, 2001
    Publication date: July 4, 2002
    Inventors: Sheng-Yueh Chang, Jiam-Hong Chen, Ting-Chun Liu, Tzu-Yu Lin, Wen-Yuang Tsai
  • Publication number: 20020031795
    Abstract: This invention concerns a compound for detecting the presence or absence of at least one microorganism. The invention also concerns the use of a compound in a detection and/or diagnostic test. The said invention further concerns a method for detecting nitroaryl reductase activity in a bacteria culture medium. Finally, the invention concerns the use of such a compound, methods for isolating and detecting microorganisms or a group of microorganisms in a sample likely to contain them, and various applications thereof.
    Type: Application
    Filed: May 4, 2001
    Publication date: March 14, 2002
    Inventors: Arthur James, Daniel Monget
  • Patent number: 6355618
    Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: March 12, 2002
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Eckard Weber, Yan Wang, Gordon B. Mills, Douglas R. Green
  • Patent number: 6344330
    Abstract: The present invention is directed to novel methods for identifying small molecule ligands that are capable of binding with high affinity to a biological target molecule of interest. High affinity binding ligands identified by the described methods find use, for example, as small molecule lead compounds that may they themselves be, or may give rise to, novel therapeutic drugs. More specifically, the subject invention is directed to methods for identifying a ligand that binds to a target biological molecule of interest, wherein a population of small organic compounds are selected and then “pre-screened” to identify those that are capable of binding to the molecular target.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: February 5, 2002
    Assignee: The Regents of the University of California
    Inventors: Jonathan A. Ellman, Ingrid Choong
  • Patent number: 6344334
    Abstract: Method for identifying a drug lead compound that inhibits binding of target bioogical molecules (TBM) by contacting TBM with members of a library of candidate cross-linked target binding fragments (CXBF), each CXBF having at least two candidate target bindig fragments (CTBF), which are inhibitors of binding, linked to a cross-linker, and selecting CXBF that inhibit the binding of the TBM to a greater extent than either of the individual CTBF linked to said cross-linker, wherein the library of CXBF is produced by: (a) screening a population of CTBF capable of being chemically cross-linked by a cross-linker to identify a subpopulation of the CTBF that inhibit binding of the TBM; and (b) chemically cross-linking members of the subpopulation of CTBF or structurally related analogs thereof with a cross-linker to provide a library of CXBF, wherein at least one linking group comprises an oxime ether linking group.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: February 5, 2002
    Assignee: The Regents of the University of California
    Inventors: Jonathan A. Ellman, Ingrid Choong
  • Patent number: 6100292
    Abstract: This invention relates to ketones represented by the following formula ##STR1## and to drugs in which such a ketone or pharmacologically acceptable salt thereof is an effective component.The ketones of the present invention encourage the production of platelets, red blood cells, white blood cells and the like, and can be used to prevent or treat cytopaenia brought about by cancer chemotherapy, radiotherapy, bone marrow transplantation and drug therapy, or by immunological abnormality or anaemia, and the like.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: August 8, 2000
    Assignee: Toray Industries, Inc.
    Inventors: Tsuyoshi Matsumoto, Hideki Kawai, Kiyoshi Okano, Katsuyuki Mori, Yasumoto Adachi
  • Patent number: 5985912
    Abstract: Compounds of the formula The compounds are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: September 18, 1998
    Date of Patent: November 16, 1999
    Assignee: Pfizer Inc.
    Inventors: Bingwei Yang, Joyce Sutcliffe, Chris J. Dutton
  • Patent number: 5951841
    Abstract: Salts of aromatic hydroxy compounds are used as brighteners in acidic electroplating baths. Furthermore, acidic electroplating baths for the electrolytic deposition of metallic layers onto shaped articles comprise, as brighteners, at least one novel salt of an aromatic hydroxy compound. Finally, shaped articles are electroplated by a process using the novel acidic electroplating baths.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: September 14, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Wehlage, Ulrich Schroder, Alfred Oftring
  • Patent number: 5877185
    Abstract: The subject invention provides for novel synergistic compositions useful for inactivating viruses or inducing apoptosis in tumor cells and for treating cancer or retroviral infections. Generally, the compositions comprise one or a plurality of ligands that oxidatively attack a zinc finger of pADPRT in combination with one or a plurality of agents selected from the group consisting of: agents that decrease cellular levels of glutathione and ligands that non-covalently bind to the nicotinamide site of pADPRT but do not effect zinc ejection from a zinc finger of pADPRT.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: March 2, 1999
    Assignee: Octamer, Inc.
    Inventors: Ernest Kun, Jerome Mendeleyev, Eva Kirsten
  • Patent number: 5830912
    Abstract: The present invention comprises 6,8-difluoro-7-hydroxycoumarins and derivatives of 6,8-difluoro-7-hydroxycoumarins, including reactive dyes, dye-conjugates and enzyme substrates. These fluorine-substituted fluorescent dyes typically possess greater photostability and lower pH sensitivity in the physiological pH range than their nonfluorinated analogs, exhibit less fluorescence quenching when conjugated to a substance, possess absorption and emission spectra that closely match those of their nonfluorinated analogs, and also exhibit higher quantum yields than their nonfluorinated analogs.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: November 3, 1998
    Assignee: Molecular Probes, Inc.
    Inventors: Kyle R. Gee, Richard P. Haugland, Wei-Chuan Sun
  • Patent number: 5767292
    Abstract: The present invention relates to processes for preparing 1-methoxy-2-propyl 3-(7-diethylamino-2-oxo-2H-chromen-3-yl)-3-oxopropionate of the formula I ##STR1## and also di(1-methoxy-2-propyl) acetonedicarboxylate as intermediate for one of the processes.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: June 16, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Peter Koch, Wolfgang Bauer
  • Patent number: 5716982
    Abstract: New retinoid compounds, as coumarin retinoids and/or purine retinoids and compositions thereof, are provided which exhibit therapeutic and/or biological activity on cancer or precancer cells, as well as to methods of use of same.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 10, 1998
    Assignee: Institute of Materia Medica, an institute of the Chinese Academy of Medical Sciences
    Inventors: Rui Han, Shi-Ping Xu
  • Patent number: 5650456
    Abstract: This invention relates to coumarin derivatives of formula (I) ##STR1## where Z represents OR.sup.3 or NR.sup.4 R.sup.5,to their preparation, and to their use for the production of polymers with luminophors on their side chains.
    Type: Grant
    Filed: February 9, 1996
    Date of Patent: July 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Chen Yun, Rolf Wehrmann, Burkhard Kohler
  • Patent number: 5624951
    Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.
    Type: Grant
    Filed: March 1, 1995
    Date of Patent: April 29, 1997
    Assignee: Pfizer Inc.
    Inventors: Bingwei Yang, Joyce Sutcliffe, Chris J. Dutton