Plural Bicyclo Ring Systems Each Having The Lactone Ring As One Of The Cyclos Patents (Class 549/284)
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Publication number: 20150111888Abstract: 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: ApplicationFiled: April 30, 2013Publication date: April 23, 2015Inventors: Ryoji Yao, Hiroyuki Osada, Yasumitsu Kondoh
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Patent number: 8729279Abstract: Agents or pharmaceutical compositions for promoting osteoblast differentiation include purified auraptene or coumarin analogs thereof represented by the following formula 1: wherein R1 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, or a carboxyethyl; R2 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, a carboxyethyl or a coumarinyl; R3 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl or a carboxyethyl; and R4 represents a hydrogen, a C1-C15 liner or branched alkyl, an alkenyl, an alkadienyl or an alkatrienyl.Type: GrantFiled: February 28, 2011Date of Patent: May 20, 2014Assignee: Erina Co., Inc.Inventors: Je-Tae Woo, Ayaka Hibino, Takayuki Yonezawa, Midori Asai, Toshiaki Teruya, Byung-Yoon Cha, Kazuo Nagai
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Publication number: 20130102796Abstract: Agents or pharmaceutical compositions for promoting osteoblast differentiation include purified auraptene or coumarin analogs thereof represented by the following formula 1: wherein R1 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, or a carboxyethyl; R2 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl, a carboxyethyl or a coumarinyl; R3 represents a hydrogen, a hydroxy, a methoxy, a methyl, an ethyl, a propyl, a carboxyl, a carboxymethyl or a carboxyethyl; and R4 represents a hydrogen, a C1-C15 liner or branched alkyl, an alkenyl, an alkadienyl or an alkatrienyl.Type: ApplicationFiled: February 28, 2011Publication date: April 25, 2013Applicant: ERINA CO., INC.Inventors: Je-Tae Woo, Ayaka Hibino, Takayuki Yonezawa, Midori Asai, Toshiaki Teruya, Byung-Yoon Cha, Kazuo Nagai
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Patent number: 8337941Abstract: The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond ? is absent and bond ? is present, or Y is H, X is CH, bond ? is present, and bond ? is absent; atom Z is a carbon and bonds ?, ? and ? are present, or is a nitrogen and bonds ?, ? and ? are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ?O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7.Type: GrantFiled: July 27, 2007Date of Patent: December 25, 2012Assignee: The Trustees of Columbia University in the City of New YorkInventors: Niko Gert Gubernator, Dalibor Sames, David Sulzer, Paul Vadola
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Patent number: 8084625Abstract: The present invention provides a crosslinking agent which have photodegradable protective groups at two ends to crosslink double-stranded nucleic acid, a nucleic acid and a protein or a polypeptide, or proteins or polypeptides, in particular, double-stranded RNA; a method for crosslinking a double-stranded RNA or the like using the same; a method for regulating gene expression, which can control the expression of a target gene at an arbitrary timing and location; and a method for examining a gene function. According to the present invention, crosslinking between double-stranded nucleic acids between a nucleic acid and a protein or a polypeptide, or between proteins or polypeptides, in particular, between double-stranded RNA can be easily formed, and in addition, the crosslinking can also be easily removed, so that the expression of a target gene can be easily controlled at an arbitrary timing and location with high efficiency.Type: GrantFiled: February 27, 2006Date of Patent: December 27, 2011Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Toshiaki Furuta, Natsuyo Imaizumi
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Patent number: 8067461Abstract: Compounds of Formula I: wherein R1, R2, M, Q and n are as defined herein, are useful as antiproliferative agents including, for example, as anticancer agents.Type: GrantFiled: June 2, 2006Date of Patent: November 29, 2011Assignee: Temple University-Of The Commonwealth System of Higher EducationInventors: M. V. Ramana Reddy, E. Premkumar Reddy
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Publication number: 20090233232Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R5 are selected from the group consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, acetoxy group, phenyl group, naphthyl group, and alkyl group in which a part or all of hydrogen atoms are substituted with fluorine atom; and X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group.Type: ApplicationFiled: May 19, 2009Publication date: September 17, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Toshiki Ito, Takako Yamaguchi
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Patent number: 7569694Abstract: Provided are an organic electroluminescent device having better performances in luminous efficiency, device life and driving voltage, a display unit equipped with the same and a lighting instrument equipped with the same. The organic electroluminescent device comprises an electron transport layer containing a specific arylamine-substituted coumarin compound.Type: GrantFiled: January 29, 2007Date of Patent: August 4, 2009Assignees: Chisso Corporation, Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Toshihiro Koike, Manabu Uchida, Makoto Satsuki, Makoto Fujiwara, Ayashi Noguchi
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Patent number: 7514158Abstract: A method for producing a coumarin compound represented by Formula 1, which comprises a step of reacting a coumarin compound represented by Formula 1 with a compound having an aldehyde group and an activated methylene group; luminous agents for organic EL elements and organic EL elements which all comprise the coumarin compound; and displaying panels and information displaying apparatuses using the organic EL elements: ø(Z)m??Formula 1 wherein in Formula 1, ø is an aromatic ring, heterocycle, or a combination thereof, each Z is the same or a different coumarin group represented by Formula 2; and m is an integer of two or more;Type: GrantFiled: December 10, 2002Date of Patent: April 7, 2009Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Makoto Satsuki, Makoto Fujiwara, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Hisato Takeuchi, Yasunori Taga
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Publication number: 20090023140Abstract: The present invention provides a crosslinking agent which have photodegradable protective groups at two ends to crosslink double-stranded nucleic acid, a nucleic acid and a protein or a polypeptide, or proteins or polypeptides, in particular, double-stranded RNA; a method for crosslinking a double-stranded RNA or the like using the same; a method for regulating gene expression, which can control the expression of a target gene at an arbitrary timing and location; and a method for examining a gene function. According to the present invention, crosslinking between double-stranded nucleic acids between a nucleic acid and a protein or a polypeptide, or between proteins or polypeptides, in particular, between double-stranded RNA can be easily formed, and in addition, the crosslinking can also be easily removed, so that the expression of a target gene can be easily controlled at an arbitrary timing and location with high efficiency.Type: ApplicationFiled: February 27, 2006Publication date: January 22, 2009Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Toshiaki Furuta, Natsuyo Imaizumi
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Publication number: 20070176544Abstract: Provided are an organic electroluminescent device having better performances in luminous efficiency, device life and driving voltage, a display unit equipped with the same and a lighting instrument equipped with the same. The organic electroluminescent device comprises an electron transport layer containing a specific arylamine-substituted coumarin compound.Type: ApplicationFiled: January 29, 2007Publication date: August 2, 2007Inventors: Toshihiro Koike, Manabu Uchida, Makoto Satsuki, Makoto Fujiwara, Ayashi Noguchi
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Patent number: 7148253Abstract: 4-Thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers are provided, as well as processes for their preparation. The invention also provides a method and composition for the treatment of hepatitis C virus (HCV) by adiministering 4-thio substituted coumarin derivatives, 4,5-dithio substituted coumarin derivatives, and coumarin dimers.Type: GrantFiled: January 6, 2004Date of Patent: December 12, 2006Assignee: XTL Biopharmaceuticals Ltd.Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu
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Publication number: 20040220258Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.Type: ApplicationFiled: April 8, 2004Publication date: November 4, 2004Inventors: Pascal Druzgala, Xiaoming Zhang, Jurg R. Pfister
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Patent number: 6770385Abstract: A fluorescent compound, suitable for use in an active layer of an organic light-emitting device and exhibiting both good luminescence and excellent thermal stability, which has the structure wherein R is substituted or unsubstituted alkyl; wherein Ar2 is optionally present; and wherein Ar1, Ar2, and Ar3 are independently each a substituted or unsubstituted aryl group.Type: GrantFiled: January 9, 2002Date of Patent: August 3, 2004Assignee: Canon Inc.Inventors: Jian Ping Chen, Travis P. S. Thoms, Bing R. Hsieh
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Patent number: 6703514Abstract: 4-thio substituted coumarin derivatives and coumarin dimers are provided, as well as processes for their preparation. A synthetic process for the preparation of 4-thio substituted coumarin derivatives is provided using mild reaction conditions, which maintains a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of 4-thio substituted coumarin derivatives for biological screening.Type: GrantFiled: May 13, 2003Date of Patent: March 9, 2004Assignee: Vivo Quest, Inc.Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu, Lisha Wang
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Publication number: 20040002538Abstract: 4-thio substituted coumarin derivatives and coumarin dimers are provided, as well as processes for their preparation. A synthetic process for the preparation of 4-thio substituted coumarin derivatives is provided using mild reaction conditions, which maintains a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of 4-thio substituted coumarin derivatives for biological screening.Type: ApplicationFiled: May 13, 2003Publication date: January 1, 2004Inventors: Jie Wu, Zhen Yang, Reza Fathi, Qiang Zhu, Lisha Wang
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Patent number: 6589976Abstract: The invention relates to novel spirocyclic phenylketoenols of the formula in which Het represents one of the groups in which Q represents and X, Y, Z, m, n, R6, R9, R10 and R11 are each as defined in the description, to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2000Date of Patent: July 8, 2003Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Markus Dollinger, Andreas Turberg
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Patent number: 6455579Abstract: Disclosed are pyran derivatives, which have distinctive sensitivity to visible light and distinctive luminous ability. The derivatives are useful in photopolymerization, electroluminescence, and dye lasers, and are obtainable through a step of reacting a compound having a 4-cyanomethylene-2-methyl-4H-pyran skeleton with a compound having a 3-formylcoumarin skeleton.Type: GrantFiled: November 9, 2000Date of Patent: September 24, 2002Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Makoto Satsuki, Akira Shinpo, Yasuyo Ooga, Sadaharu Suga, Atsushi Oda, Hiroshi Tada, Yoshikazu Sakaguchi
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Patent number: 6344334Abstract: 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: GrantFiled: March 26, 1999Date of Patent: February 5, 2002Assignee: The Regents of the University of CaliforniaInventors: Jonathan A. Ellman, Ingrid Choong
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Patent number: 6344330Abstract: 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: GrantFiled: March 27, 1998Date of Patent: February 5, 2002Assignee: The Regents of the University of CaliforniaInventors: Jonathan A. Ellman, Ingrid Choong
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Patent number: 6291518Abstract: The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: wherein R1=R2=4-hydroxycoumarin; R1=R2=4,7-dihydroxycoumarin; R1=R2=4,5,7-trihydroxycoumarin; R1=4-hydroxycoumarin, R2=—CH(OH)CH3. An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof. Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.Type: GrantFiled: January 3, 2000Date of Patent: September 18, 2001Assignee: Pliva farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventors: Mladen Trkovnik, Zrinka Ivezić
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Patent number: 6100409Abstract: The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: ##STR1## wherein R.sup.1 =R.sup.2 =4-hydroxycoumarin;R.sup.1 =R.sup.2 =4,7-dihydroxycoumarin;R.sup.1 =R.sup.2 =4,5,7-trihydroxycoumarin;R.sup.1 =4-hydroxycoumarin, R.sup.2 =--CH(OH)CH.sub.3.An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof.Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.Type: GrantFiled: October 2, 1998Date of Patent: August 8, 2000Assignee: PLIVA farmaceutska, kemijska, prehrambena i kozmeticka industrija dionicko drustvoInventors: Mladen Trkovnik, Zrinka Ivezic
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Patent number: 6034121Abstract: Compounds of the formula ##STR1## where one of Z and Y is CO and the other is C--W--R.sup.2 and the dotted line indicates a double bond is present where necessary to meet valency requirements, W is O, S(O).sub.n, N(R.sup.3), N(R.sup.3)(R.sup.4), N(R.sup.3)O or ON(R.sup.3); R.sup.1 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl group; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are as defined above for R.sup.1, or are acyl, or R.sup.2 and R.sup.3 or R.sup.2 and R.sup.4 or R.sup.3 and R.sup.4 together with the nitrogen or oxygen to which they are attached form an optionally substituted ring which may contain other hetero atoms; each X, which may be the same as or different from any other X, is halogen, CN, NO.sub.2, SF.sub.5, B(OH).sub.2, triakylsilyl or a group E, OE or S(O).sub.n E where E is a group as defined hereinbefore for R.sup.Type: GrantFiled: April 1, 1998Date of Patent: March 7, 2000Assignee: Agrevo UK LimitedInventors: Mary Josephine O'Mahony, Peter John West, Jacqueline Anne MacRitchie, Stephen David Lindell, Peter Millward
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Patent number: 5856479Abstract: Using the fluorescent group-containing carbodiimide compound represented-by the following formula (I) as the label and the like in the nucleic acid detection method, immunoassay, or chemiluminescence assay, labeling can be made efficiently for a short time, a nucleic acid derived from nature can be labelled, and highly sensitive assay is enabled.B--Y.sup.3 --N.dbd.C.dbd.N--Y.sup.2 --W--Y.sup.1 --?A!.sub.n --F(I)wherein F represents a fluorescent group;A represents a moiety selected from the group consisting of --CH.sub.2 --, --NHCO--, --CONH--, --O--, --S--, --NR-- wherein R is an alkyl group, --COO--, --OCO--, --NHSO.sub.2 --, and --SO.sub.2 NH--;n is 0 or 1;W represents a direct bond or a quaternary ammonium group;Y.sup.1, Y.sup.2 and Y.sup.3 each represents an alkylene group which may have a functional group in its main chain; andB represents H or a monovalent organic group which may be the same as or different from that represented by --W--Y.sup.1 --?A!.sub.n --F.Type: GrantFiled: May 16, 1997Date of Patent: January 5, 1999Assignee: Nisshinbo Industries, Inc.Inventors: Osamu Suzuki, Gen Masuda, Namiko Shiohata, Kazuko Matsumoto
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Patent number: 5756740Abstract: A process for the preparation of photographic binary sensitizing dyes, which comprise two separate, nonconjugated chromophores, one of which has the capability of adsorbing to a silver halide grain surface, the other of which is substantially non-adsorbing to silver halide. The process comprises reacting two dye compounds in a solvent in the presence of a 2-halo-1-alkylpyridinium salt and a 4-dialkylaminopyridine.Type: GrantFiled: April 8, 1992Date of Patent: May 26, 1998Assignee: Eastman Kodak CompanyInventors: Lal Chand Vishwakarma, Chin Hsin Chen
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Patent number: 5646164Abstract: The present inventors have discovered three classes of novel .alpha.-methylene-.gamma.-butyrolactones with excellent antiplatelet activity. As a result of intensive studies, it has been found that compounds represented by the formula I-III are potent inhibitors of platelet aggregation. ##STR1## For the formula I, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino.For the formula II, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.2 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino; R.sub.3 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino.For the formula III, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.Type: GrantFiled: November 14, 1995Date of Patent: July 8, 1997Assignee: National Science CouncilInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Tai-Chi Wang, Che-Ming Teng
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Patent number: 5116869Abstract: 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.Type: GrantFiled: September 3, 1991Date of Patent: May 26, 1992Assignee: Teijin LimitedInventors: Satoshi Sugiura, Atsuo Hazato, Toru Minoshima, Yoshinori Kato, Yasuko Koshihara, Seizi Kurozumi
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Patent number: 4547579Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atoms, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6- membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.Type: GrantFiled: September 30, 1982Date of Patent: October 15, 1985Assignee: Ciba-Geigy CorporationInventor: Peter Mockli