Pentacyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/382)
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Patent number: 6506538Abstract: The present invention relates to novel compounds of the naphthopyran type which have an annelated carbocycle in position 5,6. These compounds are of formula (I) given below: in which A is an alicyclic ring which is optionally annelated with an aromatic ring and in which two adjacent R3 can together form at least one ring, for example a benzo group. These compounds (I) possess interesting photochromic properties. The invention also relates to the method of preparing these compounds (I), as well as their applications as photochromes and compositions and (co)polymer matrices comprising them.Type: GrantFiled: September 9, 1999Date of Patent: January 14, 2003Assignee: Corning S.A.Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
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Patent number: 6506322Abstract: The present invention relates to novel naphthopyran-type compounds, annelated in position C5-C6 by an indene- or dihydronaphthalene-type carbocycle, which are of the formulae (I) and (II) given below: These compounds (I) and (II) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.Type: GrantFiled: November 14, 2000Date of Patent: January 14, 2003Assignee: Corning IncorporatedInventors: Olivier Breyne, You-Ping Chan, Patrick Jean
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Patent number: 6426023Abstract: The invention relates to novel benzopyran-type compounds having an aromatic heterocycle annelated in position 7,8 and a carbocycle annelated in position 5,6. These compounds have the formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.Type: GrantFiled: June 8, 2000Date of Patent: July 30, 2002Assignee: Corning, S.A.Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
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Patent number: 6403311Abstract: The invention relates to methods and products for analyzing polymers. The polymers are analyzed by reconstructing sequence information from population data sets. The data sets include information about polymer dependent impulses arising from the polymers. The invention is also a method for linearly analyzing polymers by assessing the intensity of a signal arising from the polymer. The signal is generated as units and/or units specific markers pass a fixed station. The quantitative intensity of the signal is proportional to the number of units and/or unit specific markers giving rise to the signal.Type: GrantFiled: August 13, 1999Date of Patent: June 11, 2002Assignee: US GenomicsInventor: Eugene Y. Chan
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Patent number: 6403812Abstract: Long wavelength, narrow emission bandwidth fluorecein dyes are provided for detecting spacially overlapping target substances. The dyes comprise 4,7-dichlorofluoresceins, and particularly 2′,4′,5′,7′-tetrachloro-4,7-dicloro-5- (and 6-) carboxyfluoresceins. Methods and kits for using the dyes in DNA analysis are provided.Type: GrantFiled: May 30, 2000Date of Patent: June 11, 2002Assignee: The Perkin-Elmer CorporationInventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam L. Woo, Steven Fung
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Patent number: 6398987Abstract: The present invention relates to novel compounds of the naphthopyran type which have a perfluoroalkyl group (X) in position 5. These compounds are of formula (I) given below: These compounds (I) possess interesting photochromic properties. The invention also relates to their preparation, their applications as photochromes as well as the compositions and matrices containing them.Type: GrantFiled: November 3, 2000Date of Patent: June 4, 2002Assignee: Corning S.A.Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
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Publication number: 20020034761Abstract: Dibenzorhodamine compounds having the structure 1Type: ApplicationFiled: October 2, 2001Publication date: March 21, 2002Applicant: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y.L. Lam, Steven Michael Menchen
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Patent number: 6326153Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitrogen and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: GrantFiled: February 14, 2001Date of Patent: December 4, 2001Assignee: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
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Patent number: 6315928Abstract: The present invention relates to specific photochromic 3H-naphtho[2,1-b]pyran derivatives and to their use in plastics of all types, especially for ophthalmic purposes. In particular, the present invention relates to spiro compounds derived from naphthopyrans and having a fluorene structure, referred to as spirofluorenopyrans, in which an annelated ring system is joined by a spiro bond to the central carbon atom of the fluorene structure.Type: GrantFiled: March 2, 2001Date of Patent: November 13, 2001Assignee: Optische Werke G. RodenstockInventors: Claudia Mann, Manfred Melzig, Udo Weigand
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Publication number: 20010039356Abstract: The invention relates to novel naphthopyran- and phenanthropyran-type compounds having a carbobicycle annelated in 5,6- position.Type: ApplicationFiled: December 29, 2000Publication date: November 8, 2001Inventors: You-Ping Chan, Patrick Jean
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Patent number: 6313161Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.Type: GrantFiled: October 26, 1999Date of Patent: November 6, 2001Assignee: Merrell Pharmaceuticals Inc.Inventors: Norton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart
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Patent number: 6296785Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which include naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the naphtho portion of the naphthopyran as shown below. Also present on the naphthopyran are moderate to strong electron donor substituents at the number 6- and 7-positions and optionally at the 8-position of the pyran ring or a cyclic group fused to the h side of the naphtho portion and weak to moderate electron donor substiuents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds have a rating of at least 80 in the Relative &Dgr;OD at Saturation Test and may be represented by the following graphic formula: Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: September 6, 2000Date of Patent: October 2, 2001Assignee: PPG Industries Ohio, Inc.Inventors: Clara M. Nelson, Anu Chopra, Olga G. Petrovskaia, David B. Knowles, Barry Van Gemert, Anil Kumar
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Publication number: 20010011139Abstract: Dibenzorhodamine compounds having the structure 1Type: ApplicationFiled: February 14, 2001Publication date: August 2, 2001Applicant: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y.L. Lam, Steven Michael Menchen
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Patent number: 6221606Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forns thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alky, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: GrantFiled: April 20, 2000Date of Patent: April 24, 2001Assignee: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
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Patent number: 6210608Abstract: The invention relates to novel naphthopyran- and phenanthropyran-type compounds having a carbobicycle annelated in 5,6-position. These compounds have formula (I) given below: These compounds (I) have interesting photochromic properties. The invention also relates to their preparation, to their applications as photochromes, as well as to the compositions and (co)polymer matrices containing them.Type: GrantFiled: February 16, 2000Date of Patent: April 3, 2001Assignee: Corning S.A.Inventors: You-Ping Chan, Patrick Jean
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Patent number: 6207084Abstract: The present invention relates to novel naphthopyrans having a cyclic group annelated in position 6,7. These naphthopyrans have formula (I) given below: These compounds (I) have advantageous photochromic properties. The invention also covers a method of preparing these naphthopyrans, as well as their applications as photochromes and compositions and (co)polymers matrices comprising them.Type: GrantFiled: September 9, 1999Date of Patent: March 27, 2001Assignee: Corning S.A.Inventors: You-Ping Chan, Patrick Jean
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Patent number: 6149841Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: December 17, 1999Date of Patent: November 21, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6146554Abstract: What is described here are photochromic naphthopyrane dyes with different substituents whose properties can be set by controlled selection of the substituents. In this manner it is possible to take an influence on the migration characteristics, the absorption characteristics and the brightening rate and kinetics. The inventive compounds display good darkening and brightening properties at a very good service life.The invention excels itself by the fact that a method is made available which is substantially improved over prior art, in addition to the surprising influence on specific properties of the inventive compounds. The described compounds are suitable for application in synthetic materials of any kind.A photochromic object is also the subject matter of the invention, which comprises one or several photochromic naphthopyrane dyes as well as at least one polymer material, with the photochromic object being producible by mass-dyeing or superficial dyeing.Type: GrantFiled: May 21, 1999Date of Patent: November 14, 2000Assignee: Optische Werke G. RodenstockInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Patent number: 6113814Abstract: Described are novel photochromic polymerizable polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one polyalkoxylated substituent of from 1 to 50 alkoxy units per substituent which is end-capped with a polymerizable group. Specific substituents are also present on the naphtho, indeno and pyrano portions of the compounds. These compounds may be represented by the following graphic formulae: ##STR1## Also described are various substrates, e.g., paper, glass, polymeric organic materials, etc., that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, indenonaphthopyrans, benzopyrans, oxazine-type compounds, etc., are also described.Type: GrantFiled: November 10, 1999Date of Patent: September 5, 2000Assignee: Transitions Optical, Inc.Inventors: Barry Van Gemert, Anu Chopra, Anil Kumar
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Patent number: 6111116Abstract: Dibenzorhodamine compounds having the structure ##STR1## are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure ##STR2## including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure ##STR3## including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, --CH.sub.2 OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodarnine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: GrantFiled: November 24, 1998Date of Patent: August 29, 2000Assignee: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
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Patent number: 6051719Abstract: Dibenzorhodamine compounds having the structure ##STR1## are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, intermediates useful for synthesizing such compounds are disclosed, such intermediates having the structure ##STR2## In Formula I, R.sub.1 is H or ##STR3## wherein Y is H, lower alkyl, lower alkene, lower alkyne, aromatic, phenyl, polycyclic aromatic, heterocycle, water-solubilizing group, or linking group, including substituted forms thereof. When R.sub.1 is H, the C-12-bonded nitrogen and the C-12 and C-13 carbons form a first ring structure having from 4 to 7 members, and/or the C-12-bonded nitrogen and the C-11 and C-12 carbons form a second ring structure having from 5 to 7 members. The compounds of Formula I further include aryl- and nitrogen-substituted forms thereof.Type: GrantFiled: November 17, 1998Date of Patent: April 18, 2000Assignee: The Perkin-Elmer CorporationInventors: Scott Conrad Benson, Joe Y. L. Lam, Krishna Gajanan Upadhya, Peggy Ann Radel, Weiguo Zhen, Steven Michael Menchen
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Patent number: 6025505Abstract: A class of 4,7-dichlororhodamine compounds useful as fluorescent dyes are disclosed having the structure ##STR1## wherein R.sub.1 -R.sub.6 are hydrogen, fluorine, chlorine, lower alkyl, lower alkene, lower alkyne, sulfonate, sulfone, amino, amido, nitrile, lower alkoxy, linking group, or combinations thereof, or, when taken together, R.sub.1 and R.sub.6 is benzo, or, when taken together, R.sub.4 and R.sub.5 is benzo; Y.sub.1 -Y.sub.4 are hydrogen or lower alkyl, or, when taken together, Y.sub.1 and R.sub.2, Y.sub.2 and R.sub.1 Y.sub.3 and R.sub.3, or Y.sub.4 and R.sub.4 is propano, ethano, or substituted forms thereof, and X.sub.1 -X.sub.3 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylate, sulfonic acid, --CH.sub.2 OH, and linking group. In another aspect, the invention includes reagents labeled with the 4,7-dichlororhodamine dye compounds, including deoxynucleotides, dideoxynucleotides, and polynucleotides.Type: GrantFiled: March 10, 1998Date of Patent: February 15, 2000Assignee: The Perkin-Elmer CorporationInventors: Linda G. Lee, Scott C. Benson, Barnett B. Rosenblum, Sandra L. Spurgeon, Jonathan M. Cassel, Ronald J. Graham
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Patent number: 6022495Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: July 10, 1998Date of Patent: February 8, 2000Assignee: Transitions Optical, Inc.Inventor: Anil Kumar
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Patent number: 6018059Abstract: The present invention has for subjects novel compounds of the [benzofuran]naphthopyran type as well as the compositions and (co)polymer matrices containing them. Said compounds possess interesting photochromic properties.Type: GrantFiled: December 3, 1997Date of Patent: January 25, 2000Assignee: Corning IncorporatedInventor: You-Ping Chan
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Patent number: 5961892Abstract: Described are novel photochromic polyalkoxylated naphthopyran compounds, examples of which are certain 2H-naphtho?1,2-b!pyrans, 3H-naphtho?2,1-b!pyrans and indeno?2,1-f!naphtho?1,2-b!pyrans, each having at least one polyalkoxylated substituent of from 2 to 50 alkoxy units per substituent. Specific substituents may also be present on the naphtho, indeno and pyrano portions of the compounds.Type: GrantFiled: September 11, 1998Date of Patent: October 5, 1999Assignee: PPG Industries Ohio, Inc.Inventors: Barry Van Gemert, Kevin J. Stewart
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Patent number: 5955520Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and having certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans and spiro(indoline)type compounds, are also described.Type: GrantFiled: June 17, 1996Date of Patent: September 21, 1999Assignee: PPG Industries, Inc.Inventors: Harry G. Heller, Julian R. Levell
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Patent number: 5936087Abstract: Dibenzorhodamine compounds having the structure ##STR1## are disclosed, including nitogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure ##STR2## including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure ##STR3## including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, --CH.sub.2 OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: GrantFiled: November 25, 1997Date of Patent: August 10, 1999Assignee: The Perkin-Elmer CorporationInventors: Scott C. Benson, Joe Y. L. Lam, Steven Michael Menchen
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Patent number: 5891368Abstract: Described are novel photochromic 8-substituted fluoranthenopyran compounds having certain substituents at the 5 position of the pyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: October 1, 1997Date of Patent: April 6, 1999Assignee: PPG Industries, Inc.Inventor: Anil Kumar
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Patent number: 5876984Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt, or a hydrate thereof, a process for preparing said compound, and a pharmaceutical composition having antiviral activity which comprise said compound.Type: GrantFiled: March 20, 1998Date of Patent: March 2, 1999Assignee: Shionogi & Co., LtdInventors: Toshiyuki Kamigauchi, Tamio Fujiwara, Hiroyoshi Tani, Yoshimi Kawamura, Isao Horibe
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Patent number: 5869658Abstract: Described are novel photochromic indeno-fused naphthopyran compounds having certain substituents at the 2-position of the pyran ring and an alkoxy group at the number 6 carbon atom. Certain other substituents may also optionally be present at the number 5, 7, 8, 9, 10, 11, 12 or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are certain novel indeno-fused naphthols which are used to make the novel naphthopyran compounds. Further described are polymeric organic host materials that contain or that are coated with the novel naphthopyran compounds, or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.Type: GrantFiled: December 15, 1997Date of Patent: February 9, 1999Assignee: PPG Industries, Inc.Inventors: Jibing Lin, Barry Van Gemert
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Patent number: 5792389Abstract: Novel water soluble dyes of the formula I are provided ##STR1## wherein R.sup.1 and R.sup.4 are alkyl of 1 to 4 carbon atoms or hydrogen; or R.sup.1 -R.sup.2 or R.sup.2 -R.sup.4 form part of aliphatic heterocyclic rings; R.sup.2 is hydrogen or joined with R.sup.1 or R.sup.4 as described above; R.sup.3 is --(CH.sub.2).sub.m --SO.sub.3.sup.-, where m is 1 to 6;X is N, CH or ##STR2## where Y is 2 --SO.sub.3.sup.- ; Z is 3, 4, 5 or 6 --SO.sub.3.sup.-. The novel dyes are particularly useful as the active media in water solution dye lasers.Type: GrantFiled: October 27, 1993Date of Patent: August 11, 1998Assignee: United States of AmericaInventors: Peter R. Hammond, James F. Feeman, George F. Field
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Patent number: 5789438Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: September 5, 1997Date of Patent: August 4, 1998Assignee: Merck & Co., Inc.Inventors: Sheo B. Singh, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink, Isabel Martin, Fernando Pelaez, Manuel Sanchez
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Patent number: 5651923Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 12, 1995Date of Patent: July 29, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5645767Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 8, 1997Assignee: Transitions Optical, Inc.Inventor: Barry Van Gemert
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Patent number: 5576424Abstract: The subject invention provides substrates useful for analyzing the metabolic activity in cells by improving the retention of a detectable reporter molecule only in intact cells where a particular enzyme is present. In particular, improved retention results from a two part process involving conjugation of haloalkyl-substituted derivatives of a reporter molecule with intracellular cysteine-containing peptides while unblocking the reporter molecule. The substrates have the formXR-SPACER-REPORTER-BLOCKwherein -BLOCK is a group selected to be removable by action of a specific analyte, to give REPORTER spectral properties different from those of the substrate,-REPORTER- is a molecule that, when no longer bound to BLOCK by a BLOCK-REPORTER bond, has spectral properties different from those of the substrate,-SPACER- is a covalent linkage, andXR- is a haloalkyl moiety that can covalently react with an intracellular thiol (Z-S-H) to form a thioether conjugate (Z-S-R-).Type: GrantFiled: November 8, 1994Date of Patent: November 19, 1996Assignee: Molecular Probes, Inc.Inventors: Fei Mao, Ram Sabnis, John Naleway, Nels Olson, Richard P. Haugland
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Patent number: 5565436Abstract: A production stimulator of nerve growth factor contains a new cyathane derivative of the form ##STR1## where R is either CHO or CH.sub.2 OH.Type: GrantFiled: October 11, 1994Date of Patent: October 15, 1996Assignee: Kagome Kabushiki KaishaInventors: Hirokazu Kawagishi, Fumihiro Ojima, Kenji Okamoto, Hideki Sakamoto, Yukio Ishiguro
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Patent number: 5536850Abstract: The present invention relates to a novel substance DC114-A1 represented by the following formula (I): ##STR1##Type: GrantFiled: March 1, 1995Date of Patent: July 16, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hirofumi Nakano, Noboru Fujii, Tamio Mizukami, Youichi Uosaki, Katsunori Kita, Eiji Kobayashi
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Patent number: 5416089Abstract: Anticancer compounds of formula I: ##STR1## and pharmaceutically acceptable salts thereof, wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected H, CH.sub.3, NH.sub.2, NO.sub.2, and CN;R.sup.9 and R.sup.10 are H or alkyl or halo, X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2, when present, join together to form, independently, a six membered 1N heterocycle substituted with 1-2 R.sup.3 ; or the group: ##STR2## wherein one of W or Z is C.dbd.O and the other is C.dbd.O, NH, S or O; or when X.sup.2 and Y.sup.2 are not joined together and when R.sup.2 is in the 4-position, then X.sup.2 and R.sup.2 may join together to form an ethylene bridge; are disclosed.Type: GrantFiled: June 24, 1993Date of Patent: May 16, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Arthur D. Patten, Gregory Pacofsky, Steven P. Seitz, Emeka A. Akamike, Robert J. Cherney, Robert F. Kaltenbach, III, Michael J. Orwat
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Patent number: 5391544Abstract: New cyathane derivatives shown by Formula (1) or (2) given below have the effect of stimulating production of nerve growth factors and antimicrobial effects: ##STR1## where R is either CHO or CH.sub.2 OH.Type: GrantFiled: February 10, 1994Date of Patent: February 21, 1995Assignee: Kagome Kabushiki KaishaInventors: Hirokazu Kawagishi, Fumihiro Ojima, Kenji Okamoto, Hideki Sakamoto, Yukio Ishiguro
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Patent number: 5294522Abstract: A novel photochromic compound as a photoreactive material making use of photochromism is provided, which compound is expressed by the following formula (1) or (2)): ##STR1## wherein R is alkyl, alkoxy, perfluoroalkyl or cyano; X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5 and X.sub.6 are each H, halogen, alkyl, alkoxy, cyano, alkanoyloxy or alkyloxycarbonyl, or a substituted or unsubstituted benzene ring is formed by condensation between at adjacent groups among X.sub.1 to X.sub.6 ; Y is Y.sub.1 C=CY.sub.2, O, S, SO, SO.sub.2 or NY.sub.3 wherein Y.sub.1 and Y.sub.2 are each as defined in the case of the above X.sub.1 to X.sub.6 and Y.sub.3 is H, alkyl, alkanoyl, alkyloxycarbonyl or aryl; and the symbol refers to occurrence of E- or Z-isomer, and which compound is useful as rewritable optical memory element or photo-display element and also as solar energy-storage material, duplicating material, masking material, optical filter, toys, etc.Type: GrantFiled: March 2, 1993Date of Patent: March 15, 1994Assignee: Chisso CorporationInventors: Manabu Uchida, Masahiro Irie
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Patent number: 5290553Abstract: A method of preparing substantially purified alkaloids from seeds, stems, uit-rind and bark of a plant selected from Picralima nitida, Gongronema latifolia, Dorstenia multiradiata, Cola attiensis, Rothmania withfieldii and Desmodium gangeticum, for use in the treatment of protozoal diseases, comprising:pulverizing said plant;a first solvent, drying the extracted material and re-extracting the dried material with a different solvent;extracting a fresh sample of said plant with boiling water;filtering and concentrating the boiling water solvent extracts under reduced pressure;concentrating the dried extract to a gum and re-extracting said gum with an aqueous acidic HCl solution;filtering the acidic extract and making it alkaline to a pH of about 9 with a concentration NaOH solution;extracting the alkaline solution with dichloromethane;concentrating organic layers of the extracted alkaline solution to dryness under reduced pressure to obtain an alkaloid fraction; andseparating the alkaloid fraction by liquid chrType: GrantFiled: July 22, 1991Date of Patent: March 1, 1994Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Maurice M. Iwu, Daniel L. Klayman, Joan E. Jackson, John D. Tally, Steven L. Andersen
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Patent number: 5284866Abstract: A compound isolated from Eupricillium brefeldionum having the structure: ##STR1## is a useful antitumor agent.Type: GrantFiled: October 5, 1992Date of Patent: February 8, 1994Assignee: Bristol-Myers Squibb CompanyInventors: Friedrich Mayerl, Xiaohua Huang, Qi Gao
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Patent number: 5188934Abstract: Long wavelength, narrow emission bandwidth fluorecein dyes are provided for detecting spacially overlapping target substances. The dyes comprise 4,7-dichlorofluoresceins, and particularly 1',2',7',8'-dibenzo-4,7-dichlorofluoresceins. Methods of using the dyes in automated DNA sequencing are described.Type: GrantFiled: November 14, 1989Date of Patent: February 23, 1993Assignee: Applied Biosystems, Inc.Inventors: Steven M. Menchen, Linda G. Lee, Charles R. Connell, N. Davis Hershey, Vergine Chakerian, Sam Woo, Steven Fung
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Patent number: 5189138Abstract: Rigid fluorine-containing compounds, monomers, and polymers based on pentacyclic core systems, such as 12H,14H-5, 7-dioxapentacene with perfluoroalkyl and/or aryl groups in the 12, 14 positions, and 5H,12H-7, 14-dioxapentacene, with perfluoroalkyl and/or aryl groups in the 5,12 positions. These monomers have utility in the preparation of advanced high-performance polymers, particularly polyimides. The rigid pentacyclic core decreases the coefficient of thermal expansion of the polymers, while the fluorinated substituents improve the dielectric constant and water absorption properties. Each monomer unit contains within its pentacyclic core two-O-bridges, and two --CRR.sub.f bridges (where R is aryl, substituted aryl or perfluoroalkyl, and R.sub.f is perfluoroalkyl).Type: GrantFiled: February 20, 1991Date of Patent: February 23, 1993Assignee: E. I. du Pont de Nemours and CompanyInventors: Swiatoslaw Trofimenko, Brian C. Auman
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2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase and 19-hydroxylase inhibitors
Patent number: 5099037Abstract: The present invention is directed to a group of compounds which are 2,19-methylenoxy or 2,19-methylenethio bridged steroids, and related steroidal compounds. These compounds are useful as aromatase and 19-hydroxylase inhibitors.Type: GrantFiled: March 25, 1991Date of Patent: March 24, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Norton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart -
Patent number: 5082857Abstract: The present invention relates to a compound designated "DC114-C" having excellent anti-bacterial and anti-tumor activities. This compound may be obtained by fermentation of a microorganism of the genus Streptomyces, preferably Streptomyces sp. DO-114 (FERM BP-2641).Type: GrantFiled: November 13, 1990Date of Patent: January 21, 1992Assignee: Kyowa Hakko Kogyo Kabushiki KaishaInventors: Hirofumi Nakano, Mitsunobu Hara, Yohichi Uosaki, Isao Kawamoto, Keiiechi Takahashi, Katsushige Gomi
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Patent number: 5021450Abstract: The present invention relates to a new class of compounds having a variable spectrum of activities for capsaicin-like responses, compositions thereof, processes for preparing the same, and uses thereof. Compounds of the invention are prepared by combining phorbol related diterpenses and homovanillac acid analogs via esterification at the exocyclic hydroxy group of the diterpene. Examples of these compounds include 20-homovanillyl-mezerein and 20-homovanillyl-12-deoxyphorbol-13-phenylacetate.Type: GrantFiled: May 30, 1989Date of Patent: June 4, 1991Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventor: Peter M. Blumberg
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Patent number: 4797421Abstract: An antioxidant containing a proanthocyanidin which is at least one member selected from the group consisting of those dimers to decimers which have bonded thereto as a structural unit a flavan-3-ol or flavan-3,4-diol represented by the general formula: ##STR1## (wherein R.sub.1 is hydrogen or a hydroxyl group, R.sub.2, R.sub.3 and R.sub.4 are each hydrogen, a hydroxyl group or a methoxy group, and R.sub.5 is hydrogen, a galloyl group or a glycopyranosil group).Type: GrantFiled: September 22, 1987Date of Patent: January 10, 1989Assignee: Kikkoman CorporationInventors: Toshiaki Ariga, Ikunori Koshiyama, Danji Fukushima
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Patent number: 4670452Abstract: There are provided benzopyrans of formula I ##STR1## wherein R.sub.6 and R.sub.7 together form the chain --CHOCH.dbd.(A.sub.1 E.sub.1)--O-- in which --O-- is attached to R.sub.7,R.sub.5 represents hydrogen,R.sub.8 represents propyl,A represents a single bond,A.sub.1 represents a single bond, phenylene or (CH.sub.2).sub.m,m represents an integer from 1 to 10 inclusive,E and E.sub.1, which may be the same or different, independently represent --COOH, 5H-tetrazolyl, or CONR.sub.24 R.sub.25, wherein R.sub.24 and R.sub.25, which may be the same or different, represent hydrogen or alkyl of C.sub.1 to C.sub.6 ;provided that when A.sub.1 represents a single bond, then E.sub.1 represents 5H-tetrazolyl or CONR.sub.24 R.sub.25, and their pharmaceutically acceptable salts, all of which are useful as anti-asthmatics.Type: GrantFiled: January 28, 1985Date of Patent: June 2, 1987Assignee: Fisons plcInventors: Kenneth J. Gould, John L. Suschitzky
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Patent number: 4429141Abstract: Physiologically active crystalline products of manufacture having the formulas: ##STR1## are described. These compounds are effective against the toxic venoms of poisonous snakes, spiders and other insects, and against E. coli endotoxins; methods are described for isolation of the above compounds.Type: GrantFiled: March 15, 1982Date of Patent: January 31, 1984Assignee: Richter Gedeon Vegyeszeti Gyar R.T.Inventors: Laszlo L. Darko, Koji Nakanishi, Masachi Nakagawa