序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
41 Methods for detecting a plurality of analytes by mass spectrometry US10008593 2001-11-09 US20020150927A1 2002-10-17 Tracy J. Matray; Vincent S. Hernandez; Ahmed Chenna; Herbert Hooper; Sharat Singh
The invention provides a method for detecting a target analyte, by: (a) contacting one or more target analytes with a set of first and second binding reagents under conditions sufficient for binding of a target analyte with the first and second binding reagents, each of the first binding reagents containing a cleavage-inducing moiety and a target binding moiety, each of the second binding reagents containing a tagged probe having a mass modifier region attached to a target binding moiety by a cleavable linkage, the cleavable linkage being susceptible to cleavage when in proximity to an activated cleavage-inducing moiety; (b) activating the cleavage-inducing moiety to release a tag reporter, and (c) detecting a mass of the tag reporter, the mass uniquely corresponding to a known target analyte.
42 Electrophoretic tag reagents comprising fluorescent compounds US10008495 2001-11-09 US20020146726A1 2002-10-10 Tracy Matray; Vincent Hernandez; Sharat Singh
Electrophoretic probes comprising fluorescent compounds as detection groups and mobility modifiers are disclosed for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. In one embodiment, detection involves the release of identifying tags as a consequence of target recognition. Target antiligands are contacted with a set of e-tag probes and the contacted antiligands are treated with a selected cleaving agent resulting in a mixture of e-tag reporters. Typically, uncleaved or partially cleaved e-tag probes are removed and the mixture of e-tag reporters is separated by any technique that provides for separation by mass or mass to charge ratio and the like and detected to provide for target identification.
43 Compositions and methods employing cleavable electrophoretic tag reagents US10008573 2001-11-09 US20020142329A1 2002-10-03 Tracy Matray; Vincent Hernandez; Sharat Singh
Probe sets for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. Detection involves the release of identifying tags as a consequence of target recognition. The probe sets include electrophoretic tag probes or e-tag probes, comprising a detection region and a mobility-defining region called the mobility modifier, both linked to a target-binding moiety. Target antiligands are contacted with a set of e-tag probes and the contacted antiligands are treated with a selected cleaving agent resulting in a mixture of e-tag reporters and uncleaved and/or partially cleaved e-tag probes. The mixture is exposed to a capture agent effective to bind to uncleaved or partially cleaved e-tag probes, followed by electrophoretic separation. In a multiplexed assay, different released e-tag reporters may be separated and detected providing for target identification. The methods employ compositions comprising luminescent molecules such as, for example, fluorescent molecules, which are modified to provide for electrophoretic properties that differ for each modified luminescent molecule while maintaining substantially the same absorption, emission and quantum yield properties of the original luminescent molecule. The compositions may be cleavably linked to binding molecules to form the e-tag probes.
44 Optical systems and methods for rapid screening of libraries of different materials US09474344 1999-12-29 US06373570B1 2002-04-16 Eric W. McFarland; Earl Danielson; William Archibald
Methods and apparatus for screening diverse arrays of materials are provided. In particular, techniques for rapidly characterizing compounds in arrays of materials in order to discover and/or optimize new materials with specific desired properties are provided. The substrate can be screened for materials having useful properties, and/or the resulting materials can be ranked, or otherwise compared, for relative performance with respect to useful properties or other characterizations. In particular, systems and methods are provided for screening a library of magnetic materials for their bulk magnetization, saturation magnetization, and coercivity by imaging their individual optical Kerr rotation, screening a library of dielectric materials for their dielectric coefficients by imaging their individual electro-optical rotation and screening a library of luminescent materials by imaging their individual luminescent properties under a variety of excitation conditions. Optical or visible luminescence systems are also provided as well as their application to screening libraries of different materials.
45 Systems and methods for characterization of materials and combinatorial libraries with mechanical oscillators US08946921 1997-10-08 US06182499B2 2001-02-06 Eric W. McFarland; Leonid Matsiev
Methods and apparatus for screening diverse arrays of materials are provided. In one aspect, systems and methods are provided for imaging a library of materials using ultrasonic imaging techniques. The system includes one or more devices for exciting an element of the library such that acoustic waves are propagated through, and from, the element. The acoustic waves propagated from the element are detected and processed to yield a visual image of the library element. The acoustic wave data can also be processed to obtain information about the elastic properties of the library element. In another aspect, systems and methods are provided for generating acoustic waves in a tank filled with a coupling liquid. The library of materials is then placed in the tank and the surface of the coupling liquid is scanned with a laser beam. The structure of the liquid surface disturbed by the acoustic wave is recorded, the recorded disturbance being representative of the physical structure of the library. In another aspect of the invention, a mechanical resonator is used to evaluate various properties (e.g., molecular weight, viscosity, specific weight, elasticity, dielectric constant, conductivity, etc.) of the individual liquid elements of a library of materials. The resonator is designed to ineffectively excite acoustic waves. The frequency response of the resonator is measured for the liquid element under test, preferably as a function of time. By calibrating the resonator to a set of standard liquids with known properties, the properties of the unknown liquid can be determined. An array of library elements can be characterized by a single scanning transducer or by using an array of transducers corresponding to the array of library elements. Alternatively, multiple resonators of differing design may be used to evaluate each element of a library of elements, thus providing improved dynamic range and sensitivity.
46 Mass spectrometers and methods for rapid screening of libraries of different materials US946730 1997-10-08 US5959297A 1999-09-28 W. Henry Weinberg; Eric W. McFarland; Peijun Cong; Shenheng Guan
Methods and apparatus for screening diverse arrays of materials are provided. Techniques are provided for rapidly characterizing compounds in combinatorial arrays of materials for discovering and/or optimizing new materials with specific desired properties. A scanning mass spectrometer is used which includes an ionization chamber and a collector that outputs an electrical signal responsive to the quantity of gas ions contacting the collector surface. A conduit system selectively withdraws samples from the array of materials, passing the samples into the ionization chamber. In a specific embodiment, reactants are passed through the conduit system to the selected regions of interest on the substrate.
47 포유류 아난다미드 운반물질을 억제하는 아민, 및 이의사용 방법 KR1020047018474 2003-05-15 KR101087883B1 2011-11-30 아큐일라,브라이언,에이.; 홉킨스,세드; 록신,커티스,에이.; 왕,펭지앙
본 발명의 일면은 아민에 관한 것이다. 본 발명의 또 다른 일면은 포유류 아난다미드 운반물질의 억제제로서의 아민의 용도에 관한 것이다. 본 발명의 화합물은 천식, 신경병적 통증, 지속통, 염증성 통증, 과잉운동증, 고혈압, 뇌허혈, 파킨슨병, 근긴장, 뚜레 증후군, 정신분열증, 출혈성 쇼크, 패혈성 쇼크, 편두통, 집락성 두통, 다발성 경화증, 식욕결핍증, AIDS 소모성 증후군, 장기 거부반응, 자가면역 질병, 알레르기, 관절염, 크론병, 악성 신경교종, 신경퇴행성 질병, 헌팅턴 무도병, 녹내장, 메스꺼움, 불안증, 정신병, 주의력 결핍 과잉행동 장애, 조루증 또는 뇌졸중을 포함하지만 이들에 제한되지 않는, 포유류에 고통을 주는 다수의 병, 질환 및 질병을 치료하는 데에 또한 사용된다.
48 포유류 아난다미드 운반물질을 억제하는 아민, 및 이의사용 방법 KR1020047018474 2003-05-15 KR1020050012246A 2005-01-31 아큐일라,브라이언,에이.; 홉킨스,세드; 록신,커티스,에이.; 왕,펭지앙
본 발명의 일면은 아민에 관한 것이다. 본 발명의 또 다른 일면은 포유류 아난다미드 운반물질의 억제제로서의 아민의 용도에 관한 것이다. 본 발명의 화합물은 천식, 신경병적 통증, 지속통, 염증성 통증, 활동항진, 고혈압, 뇌허혈, 파킨슨병, 근긴장, 뚜레 증후군, 정신분열증, 출혈성 쇼크, 패혈성 쇼크, 편두통, 집락성 두통, 다발성 경화증, 식욕결핍증, AIDS 소모성 증후군, 장기 거부반응, 자기면역 질병, 알레르기, 관절염, 크론병, 악성 신경교종, 신경퇴행성 질병, 헌팅턴 무도병, 녹내장, 메스꺼움, 불안증, 정신병, 주의력 결핍 과잉행동 장애, 조루증 또는 뇌졸중을 포함하지만 이들에 제한되지 않는, 포유류에 고통을 주는 다수의 병, 질환 및 질병을 치료하는 데에 또한 사용된다.
49 택 라이브러리 화합물, 조성물, 키트 및 사용 방법 KR1020027014399 2000-10-27 KR1020030032939A 2003-04-26 싱샤럿; 맷레이트레이시; 살린미-무사비후세인
조성물의 패밀리가 표지로서 제공되며, 이것은 중합체 화합물에 부착되고, 중합체 화합물로부터 eTag 리포터의 유리 및 분리 및 검출을 기초로 분석하는 eTag 리포터로 언급된다. 올리고뉴클레오티드에 대해서, eTag 리포터는 포스파이트 또는 포스페이트 화학을 사용함에 의해 올리고뉴클레오티드의 단부에서 합성되며, 이로써 질량-변경 영역, 전하-변경 영역 및 검출가능한 영역이 연속적으로 부가되어 eTag 표지된 리포터를 생성한다. 작은 빌딩블록 및 변화하는 그것들의 조합을 사용함에 의해, 다수의 상이한 eTag 리포터가 쉽게 생성되고, 확인을 위해 관심의 올리고뉴클레오티드에 부착될 수 있다. 표적 서열이 샘플에 존재할 때 eTag 리포터를 유리시키는 프로토콜이 사용된다.
50 Alternative nucleic acid sequencing methods EP13168115.7 2008-08-28 EP2657869A3 2015-06-03 Bortner, Scott R.

Embodiments are provided that provide for parallel sequencing of nucleic acid segments. In some embodiments, a single sequence is sequenced by at least two different sequencing techniques and the results compared, allowing for deficiencies or strengths of one technique to be complemented by the second technique.

51 Alternative nucleic acid sequencing methods EP13168115.7 2008-08-28 EP2657869A2 2013-10-30 Bortner, Scott R.

Embodiments are provided that provide for parallel sequencing of nucleic acid segments. In some embodiments, a single sequence is sequenced by at least two different sequencing techniques and the results compared, allowing for deficiencies or strengths of one technique to be complemented by the second technique.

52 PEPTIDE LIBRARIES FOR SCREENING AND OTHER APPLICATIONS EP11820266.2 2011-08-29 EP2609236A1 2013-07-03 LEE, Su Seong; LIM, Jaehong; CHA, Junhoe; ANG, Yi Li; ZHENG, Yiran; TAN, Sylvia
The present invention generally relates to various peptides and particles, for example, for use in screening of particle- or bead-based peptide libraries. In one aspect, the present invention is generally directed to articles including peptides attached to one or more particles, which may have structures such as (particle)-M-Q-Z n-X-J, (particle)-M-Q-Z n-X 1-X 2-X 3-X 4-X 5-J, (particle)-M-R-Z n-X 1-X 2-X 3-X 4-X 5-J, (particle)-M-R- -X 1-X 2-X 3-X 4-X 5-Z n-Q-J, (particle)-M-X 1-X 2-X- 3X 4-X 5-Z n-R-J, etc., where M is a methionine residue, M1 is a cleavable linker residue, Q is a group able to enhance intensity and/or sensitivity of mass spectrometry, X comprises one or more amino acid residues, n is a positive integer, Z is a covalent bond or a spacer, and J is an endgroup. In some embodiments, the spacer may comprise a structure such as:(I). Other aspects of the present invention generally relate to methods of using such articles, e.g., by exposing the article to a target molecule such as a protein, for example, for use in screening of particle-based peptide libraries. Still other aspects of the present invention generally relate to methods of making such articles, methods of promoting such articles, kits involving such articles, or the like.
53 Methods for ligand discovery EP08006555.0 2002-04-24 EP1939625A2 2008-07-02 Erlanson, Daniel A.; Braisted, Andrew, C.; Wells, James

The present invention provides novel methods for ligand discovery. The inventive methods rely on a process termed "tethering" where potential ligands are covalently bonded or "tethered" to a target and subsequently identified.

54 Methods for multiplexed determination of target species using tag library compounds, compositions and kits EP00973963.2 2000-10-27 EP1278760B1 2008-06-11 SINGH, Sharat; MATRAY, Tracy; SALINMI-MOOSAVI, Hussein
Families of compositions are provided as labels, referred to as eTag reporters for attaching to polymeric compounds and assaying based on release of the eTag reporters from the polymeric compound and separation and detection. For oligonucleotides, the eTag reporters are synthesized at the end of the oligonucleotide by using phosphiste or phosphate chemistry, whereby mass-modifying regions, charge-modifying regions and detectable regions are added sequentially to produce the eTag labeled reporters. By using small building blocks and varying their combination large numbers of different eTag reporters can be readily produced attached to the oligonucleotide of interest for identification. Protocols are used that release the eTag reporter when the target sequence is present in the sample.
55 INFRARED SPECTROSCOPY AND IMAGING OF LIBRARIES EP97910844.6 1997-10-07 EP0934515B1 2006-03-08 McFARLAND, Eric, W.; ARCHIBALD, William
Methods and apparatus for screening diverse arrays of materials using infrared imaging techniques are provided. Typically, each of the individual materials on the array will be screened or interrogated for the same material characteristic. Once screened, the individual materials may be ranked or otherwise compared relative to each other with respect to the material characteristic under investigation. According to one aspect, infrared imaging techniques are used to identify the active sites within an array of compounds by monitoring the temperature change resulting from a reaction. This same technique can also be used to quantify the stability of each new material within an array of compounds. According to another aspect, identification and characterization of condensed phase products is achieved, wherein library elements are activated by a heat source serially, or in parallel. According to another aspect, a Fourier transform infrared spectrometer is used to rapidly characterize a large number of chemical reactions contained within a combinatorial library.
56 AMINES THAT INHIBIT A MAMMALIAN ANANDAMIDE TRANSPORTER, AND METHODS OF USE THEREOF EP03736639.0 2003-05-15 EP1509489A1 2005-03-02 AQUILA, Brian, A.; HOPKINS, Seth; LOCKSHIN, Curtis, A.; WANG, Fengjiang
One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson’s disease, spasticity. Tourette’s syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton’s headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn’s disease, malignant gliomas, neurodegenerative diseases, Huntington’s chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.
57 Verfahren zum Verifizieren der Synthese organischer Moleküle in der kombinatorischen Chemie EP99119836.7 1999-10-07 EP1000918A3 2004-09-29 Schröder, Harald, Dr.; Neidig, Klaus-Peter, Dr.

Ein Verfahren zum Verifizieren der Synthese von aus Substrukturen aufgebauten organischen Molekülen der kombinatorischen Chemie umfaßt folgende Schritte:

  • (A) Bereitstellung der Substrukturen der organischen Moleküle und Zuordnen von Substrukturcodes (Ax, By, Cz, ...);
  • (B) Synthese der organischen Moleküle, die diese Substrukturen enthalten, durch systematisches Kombinieren von unterschiedlichen Substrukturen und jeweils Zuordnung eines Gesamtcodes für die jeweilige Kombination;
  • (C) Aufnahme von mehrdimensionalen NMR-Spektren der synthetisierten organischen Moleküle;
  • (D) eindeutige Zuordnung von Signalyruppen der NMR-Spektren zu den einzelnen Substrukturen;
  • (E) Überprüfung der NMR-Spektren der Kombinationen auf das Vorhandensein aller zugeordneten Signalgruppen.

Damit wird eine schnelle, reproduzierbare und zuverlässige Verifizierung einer großen Anzahl von systhetisierten Produkten der kombinatorischen Chemie ermöglicht.

58 CHEMICAL CONSTRUCTS EP99947750.8 1999-10-05 EP1119529B1 2003-09-17 CARR, Robin, Arthur, Ellis c/o Glaxo Wellcome plc; GEHANNE, Sylvie Glaxo Wellcome SpA; KAY, Corinne c/o Glaxo Wellcome Chemistry Lab.; McKEOWN, Stephen, Carl Glaxo Wellcome plc; MURRAY, Peter, John OSI Pharmaceuticals; PAIO, Alfredo Glaxo Wellcome SpA; SCICINSKI, Jan c/o Glaxo Wellcome Chemistry Lab.; WATSON, Stephen, Paul Glaxo Wellcome plc; WILLIAMS, G. c/o Glaxo Wellcome Chemistry Lab.; ZARAMELLA, Alessio Glaxo Wellcome SpA
The invention provides a chemical construct for use in solid phase synthesis comprising a solid support Q having linked thereto via a connecting group Y a substrate R; the connecting group Y having first and second cleavage sites which are orthogonally and selectively cleavable; the second cleavage site being selectively cleavable to release the substrate; and the first cleavage site being located at a position between the second cleavage site and the solid support and being selectively cleavable to release a fragment Fr comprising the substrate and at least a portion of the connecting group Y; characterised in that cleavage at the first cleavage site forms or introduces on the chemical fragment Fr at the first cleavage site a moiety comprising a sensitising group G (such as an amino group) which sensitises the chemical fragment Fr to instrumental, e.g. mass spectroscopic, analysis. Also provided are methods of analysis employing the constructs, as well as intermediate constructs.
59 A METHOD FOR PREPARING AND SCREENING ONE OR MORE COMPOUNDS EP00962771.2 2000-10-06 EP1222152A1 2002-07-17 WILLIAMS, Lorenzo
A method for sequentially performing a synthesis, separation and screening of chemical entities, especially a combinatorial library, is described. The method utilises a bulk of a stationary phase (e.g. silica gel, aluminium oxide, cellulose, etc. for example arranged on a backing) for the performance of the synthesis, separation and screening. The technique described enables a rapid route from synthesis to the testing of chemical compounds. Screening can be performed without need for reaction work-up. Preferred screening methods are those used to determine the biological activity of the compounds.
60 ANTISENSE MODULATION OF PTEN EXPRESSION EP99966206.7 1999-12-14 EP1200456A1 2002-05-02 MONIA, Brett, P.; COWSERT, Lex, M.
Antisense compounds, compositions and methods are provided for modulating the expression of PTEN. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding PTEN. Methods of using these compounds for modulation of PTEN expression and for treatment of diseases associated with expression of PTEN are provided.
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