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111. 发明公开

EP1301485A1 ACRIDIN-DERIVATE UND DEREN VERWENDUNG ALS ARZNEIMITTEL 有权
标题翻译：吖啶衍生物及其作为药物
公开(公告)号：EP1301485A1
公开(公告)日：2003-04-16
申请号：EP01969410.8
申请日：2001-07-18
申请人： Zentaris AG
发明人： EMIG, Peter , GÜNTHER, Eckhard , BAASNER, Silke , BACHER, Gerald , BECKERS, Thomas , AUE, Beate
IPC分类号： C07D219/04 , A61K31/473 , A61P35/00
CPC分类号： C07D219/04
摘要： The invention relates to novel acridine derivatives of general formula (1), the production thereof and the use of the same as pharmaceuticals, especially for treating tumours.

112. 发明授权

EP0625510B1 Novel N-alkylacridan carboxyl derivatives useful for chemiluminescent detection 失效
标题翻译：的N- Alkylacridancarboxylderivate，适合于通过化学发光检测
公开(公告)号：EP0625510B1
公开(公告)日：2003-04-02
申请号：EP94107632.5
申请日：1994-05-17
申请人： LUMIGEN, INC.
发明人： Akhavan-Tafti, Hashem , Desilva, Renuka , Sugioka, Katsuaki
IPC分类号： C07D219/04 , G01N33/58 , C12Q1/28
CPC分类号： C12Q1/28 , C07D219/02 , C07D219/04 , C07D219/06 , Y10S435/81 , Y10S435/968

113. 发明授权

EP0754178B1 NOVEL FUNCTIONALIZED HYDROPHILIC ACRIDINIUM ESTERS 失效
标题翻译：功能化的亲水性吖啶酯
公开(公告)号：EP0754178B1
公开(公告)日：2003-01-15
申请号：EP95913298.6
申请日：1995-04-06
申请人： Bayer Corporation
发明人： LAW, Say-Jong , SOTIRIOU-LEVENTIS, Chariklia , NATRAJAN, Anand , JIANG, Qingping , CONNOLLY, Peter, B. , KILROY, John, P. , MCCUDDEN, Constance, R. , TIRRELL, Stephen, M.
IPC分类号： C07D219/04 , G01N33/533 , G01N33/58 , C07J43/00
CPC分类号： C07D401/12 , C07D219/04 , C07F9/64 , C07J1/0011 , C07J1/0022 , C07J21/006 , C07J43/003 , C12Q1/6816 , G01N33/533 , G01N33/586 , C12Q2563/161 , C12Q2563/103
摘要： Novel acridinium esters that are useful, either alone or when incorporated into liposomes, as chemiluminescent agents in binding assays (e.g., immunoassays and gene probe assays) with improved sensitivity are disclosed. In addition, the synthesis of these esters and their use in assays for detecting an analyte is described. In particular, assays for testosterone and the Rubella virus are disclosed.

114. 发明公开

EP1234514A3 A reduced ignition propensity smoking article 有权
标题翻译：一种烟制品，以减少引燃倾向
公开(公告)号：EP1234514A3
公开(公告)日：2003-01-02
申请号：EP01304017.5
申请日：2001-05-02
申请人： Lorillard Licensing Company, Llc
发明人： Grider, David A. , Jessup, Terry D. , Williams, David L. , Zawadzki, Michael A. , Ihrig, Arthur M.
IPC分类号： A24D1/02
CPC分类号： C07D409/04 , A24D1/025 , C07D219/04 , C07D219/06 , C07D411/04 , C07F9/64
摘要： A smoking article having reduced ignition propensity is disclosed. The smoking article (10) includes a tobacco column (12), a wrapper (14) surrounding the tobacco column and a filter element (16). The wrapper has a base permeability, and untreated areas (20) alternating with discrete areas (22) treated with a composition to reducing the base permeability. The discretely treated areas (22) interact with a coal of a burning tobacco firecone as it advances to self-extinguish the smoking article. The composition of the treated areas includes a permeability reducing substance, a burn rate retarding substance and a burn rate accelerating substance. Either the burn rate retarding substance or the burn rate accelerating substance acts as an organoleptic enhancing substance. In this way a smoker's experience when smoking either the treated areas or the untreated areas is substantially the same.

115. 发明公开

EP1234514A2 A reduced ignition propensity smoking article 有权
标题翻译： Rauchartikel mit herabgesetzterZündungsneigung
公开(公告)号：EP1234514A2
公开(公告)日：2002-08-28
申请号：EP01304017.5
申请日：2001-05-02
申请人： Lorillard Licensing Company, Llc
发明人： Grider, David A. , Jessup, Terry D. , Williams, David L. , Zawadzki, Michael A. , Ihrig, Arthur M.
IPC分类号： A24D1/02
CPC分类号： C07D409/04 , A24D1/025 , C07D219/04 , C07D219/06 , C07D411/04 , C07F9/64
摘要： A smoking article having reduced ignition propensity is disclosed. The smoking article (10) includes a tobacco column (12), a wrapper (14) surrounding the tobacco column and a filter element (16). The wrapper has a base permeability, and untreated areas (20) alternating with discrete areas (22) treated with a composition to reducing the base permeability. The discretely treated areas (22) interact with a coal of a burning tobacco firecone as it advances to self-extinguish the smoking article. The composition of the treated areas includes a permeability reducing substance, a burn rate retarding substance and a burn rate accelerating substance. Either the burn rate retarding substance or the burn rate accelerating substance acts as an organoleptic enhancing substance. In this way a smoker's experience when smoking either the treated areas or the untreated areas is substantially the same.
摘要翻译：公开了具有降低的点火倾向的吸烟制品。吸烟制品（10）包括烟草柱（12），围绕烟草柱的包装（14）和过滤元件（16）。包装物具有基础渗透性，并且未处理区域（20）与用组合物处理以降低基础渗透性的离散区域（22）交替。离散处理区域（22）与燃烧的烟草火鸡的煤相互作用，因为它前进以自动熄灭吸烟物品。处理区域的组成包括渗透率降低物质，燃烧速率阻滞物质和燃烧速度加速物质。燃烧速率缓慢物质或燃烧速率加速物质都可以用作感官增强物质。以这种方式，吸烟者在经过治疗的地区或未经治疗的地区吸烟时的经验基本相同。

116. 发明授权

EP0915851B1 DIBENZODIHYDROPYRIDINECARBOXYLIC ESTERS AND THEIR USE IN CHEMILUMINESCENT ASSAY METHODS 失效
标题翻译： Dibenzodihydropyridinecarboxylic酯及其化学发光INVESTIGATIONS应用
公开(公告)号：EP0915851B1
公开(公告)日：2002-03-20
申请号：EP97930881.4
申请日：1997-07-15
申请人： DE STAAT DER NEDERLANDEN VERTEGENWOORDIGD DOOR DE MINISTER VAN WELZIJN, VOLKSGEZONDHEID EN CULTUUR
发明人： JACQUEMIJNS, Marjorie , ZOMER, Gijsbert
IPC分类号： C07D219/04 , G01N33/58 , C07D221/12
CPC分类号： C07D221/12 , C07D219/04 , C12Q1/28 , Y10S435/968 , Y10S435/975
摘要： New dibenzodihydropyridinecarboxylic esters are provided which comply with formula (1) or (2), wherein: R1 is substituted alkyl or cyano; R?2 and R3¿ are independently hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R4 is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R?5 and R6¿ are indenpendently alkyl, alkoxy or another substituent which is relatively resistant to oxidation; m and n are integers from 0 to 4; wherein, if m or n is at least 2, two groups R5 or R6 may be linked together; and Z is oxygen or sulphur. The new compounds are useful as chemiluminogenic reagents for detecting the presence of peroxidase activity at extremely low levels (10-20 moles).

117. 发明公开

EP1173414A1 N-PROTECTED AMINES AND THEIR USE AS PRODRUGS 审中-公开
标题翻译： N-GESCHÜTZTEAMINE UND IHRE VERWENDUNG ALS PRODRUGS
公开(公告)号：EP1173414A1
公开(公告)日：2002-01-23
申请号：EP00925489.7
申请日：2000-04-26
申请人： CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED
发明人： DENNY, William Alexander,Auckland Cancer Society , HAY, Michael Patrick,Auckland Cancer Society , WILSON, William Robert,Department of Pathology
IPC分类号： C07C271/28 , C07C271/24 , C07C271/20 , C07D219/04 , C07D219/08 , C07D209/60 , C07D233/91 , C07D233/92 , C07D277/66 , C07D307/71 , C07D333/44 , C07D231/16 , A61K31/27 , A61K31/435 , A61K31/40
CPC分类号： C07D333/44 , C07C271/20 , C07C271/28 , C07C2603/24 , C07D209/60 , C07D219/04 , C07D219/08 , C07D231/16 , C07D233/91 , C07D233/92 , C07D277/66 , C07D307/71 , Y02P20/55
摘要： Compounds of formula (I) or (II), wherein X represents H, C1-6 alkyl or C1-6 alkoxy, said alkyl or alkoxy being optionally substituted with one or more groups; a is 0,1,2,3 or 4; Y represents H or C1-6 alkyl; 1, 2 or 3 of the members Z of the 5-membered aromatic ring are independently selected from -O-, -S-, -N= or -NR-, where R is H or C1-6 alkyl optionally substituted with one or more of groups; and E represents a moiety such that EH is an amine; provided that in formula (I) if a = 0 then Y≠H, are provided along with a method of selecting desired protecting groups by measuring the fragmentation rates of compounds of formula (I) or (II) when the nitro group is selected.
摘要翻译：式（I）或（II）的化合物，其中X表示H，C 1-6烷基或C 1-6烷氧基，所述烷基或烷氧基任选被一个或多个基团取代; a为0,1,2,3或4; Y表示H或C 1-6烷基; 1，2或3个5元芳环的成员Z独立地选自-O - ， - S - ， - N =或-NR-，其中R是H或任选地被一个或多个更多的团体 E表示EH为胺的部分; 条件是在式（I）中，如果a = 0则Y≠H，以及当选择硝基时通过测量式（I）或（II）化合物的断裂速率来选择所需保护基团的方法提供。

118. 发明公开

EP1121342A1 DIAMINOPROPIONIC ACID DERIVATIVES 审中-公开
标题翻译： DIAMINOPROPIONSURE衍生
公开(公告)号：EP1121342A1
公开(公告)日：2001-08-08
申请号：EP99953772.3
申请日：1999-10-12
申请人： F. HOFFMANN-LA ROCHE AG
发明人： FOTOUHI, Nader , GILLESPIE, Paul , GUTHRIE, Robert, William , PIETRANICO-COLE, Sherrie, Lynn , YUN, Weiya
IPC分类号： C07C235/52 , C07C233/83 , C07D333/40 , C07D333/38 , C07D249/18 , C07D209/08 , A61K31/166 , A61K31/33 , A61P7/00 , C07C233/63 , C07D213/56 , C07C233/78
CPC分类号： C07D295/15 , C07C65/105 , C07C65/40 , C07C233/65 , C07C233/66 , C07C233/73 , C07C233/83 , C07C235/34 , C07C235/52 , C07C235/60 , C07C237/12 , C07C237/20 , C07C237/24 , C07C237/36 , C07C255/57 , C07C271/22 , C07C271/24 , C07C271/28 , C07C311/06 , C07C311/19 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2603/18 , C07C2603/74 , C07D207/16 , C07D209/08 , C07D209/16 , C07D209/20 , C07D209/34 , C07D209/42 , C07D211/62 , C07D211/88 , C07D213/78 , C07D215/48 , C07D215/54 , C07D217/26 , C07D219/04 , C07D223/12 , C07D223/16 , C07D223/20 , C07D237/28 , C07D241/44 , C07D249/20 , C07D261/18 , C07D277/06 , C07D277/46 , C07D277/54 , C07D277/56 , C07D285/06 , C07D307/68 , C07D311/08 , C07D311/24 , C07D333/28 , C07D333/38 , C07D335/16 , C07D409/12 , C07D471/04
摘要： Compounds of the formula (1a), wherein R1 is a group of the formula (2) where R1, R2, A, B, U, V, W, X, Y, Z, k and n have the significance given in the specification, are useful to treat rheumatoid arthritis, psoriasis, multiple sclerosis, Crohn's disease, ulcerative colitis, artherosclerosis, restenosis, pancreatitis, transplant rejection, delayed graft function and diseases of ischemia reperfusion injury, including acute myocardial infarction and stoke.
摘要翻译：式Id的化合物及其药学上可接受的盐和酯，其中取代基名称如说明书中所提供。本发明的化合物可用于治疗再灌注损伤。

119. 发明公开

EP1104405A1 NEAR INFRARED CHEMILUMINESCENT ACRIDINIUM COMPOUNDS AND USES THEREOF 有权
标题翻译：中红外化学发光吖啶衍生物及其
公开(公告)号：EP1104405A1
公开(公告)日：2001-06-06
申请号：EP99941005.3
申请日：1999-08-10
申请人： Bayer Corporation
发明人： NATRAJAN, Anand , JIANG, Qingping , SHARPE, David , LAW, Say-Jong
IPC分类号： C07D219/04 , G01N33/58 , G01N33/533
CPC分类号： G01N33/582 , C07D219/04 , Y10S436/80 , Y10S436/815 , Y10S436/817 , Y10S530/812 , Y10T436/13
摘要： Our results thus identify two sets of necessary and sufficient criteria for observing long-wavelength emission from acridinium compounds: Set A: (a) the creation of an extended conjugation system by the attachment of appropriate functional groups on the acridinium nucleus (electronic requirement). (b) Coplanarity of the attached functional group and the acridone moiety during light emission (geometry requirement). (c) Said functional group must consist of at least one aromatic ring and one electron-donating atom or group with an extra pair of electrons which can readily delocalize into the extended π system to which the heteroatom is directly attached or built into, and establish stable extended resonance with the electron-withdrawing carbonyl moiety of the light emitting acridone. Such electron-donating atom or group that exists in the form of an anion has particularly strong effect to further the bathochromic shift of the emission wavelength. Set B: (a) A direct attachment at one or more of positions C-2, C-4, C-5, or C-7 of the acridinium nucleus, of electron-donating atoms or groups having extra pair(s) of electrons. The electron-donating entities can be the same or different if more than one electron-donating entity is used. Such electron-donating atom or group that exists in the form of an anion has particularly strong effect to further the bathochromic shift of the emission wavelenth. For molecules for which the above criteria are met such as LEAE, 3-HS-DMAE, and 2-hydroxy-DMAE long wavelength-emission exceeding 500 nm and reaching into NIR region is expected and observed. Preferably, the utility of an NIR-AC of comparable quantum yield as the conventional acridinium compounds goes hand-in-hand with the employment of a luminescence detector of good to excellent detection efficiency. To achieve efficient NIR signal detection and facilitate the performing of diagnostic assays, a further objective of the present invention is the advance of a concept and the realization of substituting a state-of-the-art charge-coupled device (CCD) detector for the red-insensitive photomultiplier tube (PMT) in a conventional fully or semi-automatic analyzer such as MLA-II of Chiron Diagnostics, Walpole, MA.

120. 发明公开

EP0938677A4 CHEMILUMINESCENT DETECTION METHODS USING DUAL ENZYME-LABELED BINDING PARTNERS 失效
标题翻译： CHEMILUMINESZENDE检测方法用两种酶标记的结合伴侣
公开(公告)号：EP0938677A4
公开(公告)日：2000-09-27
申请号：EP97913856
申请日：1997-11-07
申请人： LUMIGEN INC
发明人： AKHAVAN-TAFTI HASHEM , SUGIOKA KATSUAKI , SUGIOKA YUMIKO , REDDY LEKKALA V
IPC分类号： G01N33/535 , C07D219/02 , C07D219/04 , C07D219/06 , C09B15/00 , C09K11/07 , C12Q1/28 , C12Q1/34 , C12Q1/68 , G01N21/78 , G01N33/53 , G01N33/543 , G01N33/58
CPC分类号： C07D219/02 , C07D219/04 , C07D219/06 , C09B15/00 , C12Q1/28 , G01N33/581 , G01N33/582
摘要： Methods of detecting analytes or target species using two enzyme-labeled specific binding partners where the two enzymes function in concert to produce a detectable chemiluminescent signal are disclosed. The methods use a specific binding partner labeled with a hydrolytic enzyme to produce a phenolic enhancer in close proximity to a peroxidase-labeled second specific binding partner. The method is useful to detect and quantitate with improved specificity various biological molecules including antigens and antibodies by the technique of immunoassay, proteins by Western blotting, DNA by Southern blotting, RNA by Northern blotting. The method may also be used to detect DNA mutations and juxtaposed gene segments in chromosomal translocations and particularly to unambiguously identify heterozygous genotypes in a single test.

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