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公开(公告)号：US5612002A
公开(公告)日：1997-03-18
申请号：US430696
申请日：1995-04-28
申请人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
发明人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , B01J8/00 , C07K17/00 , C12M1/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： A method for the multiple, simultaneous synthesis of compounds comprising the steps of: 1) providing an apparatus comprising a plurality of reaction tubes having filter members on their lower ends, a reservoir member for receiving the filter member, a holder member having a plurality of apertures for supporting the reaction tubes, and a manifold member adjacent to the holder member and enclosing the upper ends of the reaction tubes; 2) charging the apparatus with reactants required for synthesis; 3) synthesizing the compounds in solution; or optionally 4) cleaving the compounds from a solid support within the apparatus.
摘要翻译： 一种用于多次同时合成化合物的方法，包括以下步骤：1）提供一种装置，包括在其下端具有多个具有过滤器构件的反应管，用于容纳过滤构件的储存器构件，具有多个 用于支撑反应管的孔，以及与保持器构件相邻并包围反应管的上端的歧管构件; 2）用合成所需的反应物对设备进行充电; 3）在溶液中合成化合物; 或任选地4）在装置内从固体支持物上切割化合物。
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公开(公告)号：US5324483A
公开(公告)日：1994-06-28
申请号：US12557
申请日：1993-02-02
申请人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
发明人： Donna R. Cody , Sheila H. H. DeWitt , John C. Hodges , John S. Kiely , Walter H. Moos , Michael R. Pavia , Bruce D. Roth , Mel C. Schroeder , Charles J. Stankovic
IPC分类号： B01J19/00 , C07B61/00 , C07C275/28 , C07K1/04 , C07K5/062 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14 , C08F283/00
CPC分类号： C07K1/047 , B01J19/0046 , C07K1/045 , B01J2219/00283 , B01J2219/00308 , B01J2219/0031 , B01J2219/00373 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00493 , B01J2219/00495 , B01J2219/005 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00689 , B01J2219/00695 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , C40B40/06 , C40B40/10 , C40B50/14 , C40B60/14
摘要： An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
摘要翻译： 提供合适的位置用于多次同时合成化合物的装置和方法。 该装置包括：具有多个井的储存器块; 多个反应管，通常为气体分散管，在其下端具有过滤器; 具有多个孔的保持器块; 以及可以具有允许引入/维护受控环境的端口的歧管。 歧管顶壁具有孔和具有相同孔的可拆卸板。 该装置由适应加热，冷却，搅拌或腐蚀性试剂的材料构成。 垫片放在组件之间。 提供杆或夹具用于将部件固定在一起。 设备操作涉及将过滤器放置在储存器块井中的反应管的下端，并且通过保持器的上端阻挡孔并进入歧管。 该装置提供超过1mg每种产品的结构知识和对每种化合物的控制。 使用该装置，一系列构建块共价连接到固体支持物上。 然后通过共价添加其他不同的构建块或化学修饰一些现有功能来修改这些构建块，直到实现倒数第二个结构。 然后通过另一种化学反应将固体支持物从该固体支持物中裂解成孔内的溶液，得到新合成的单独化合物的阵列，其在反应后修饰（如果需要）适于测试活性。
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3.发明授权Azabicyclo and azacyclo oxime and amine cholinergic agents and methods of treatment 失效氮杂双环和吖嗪肟和胺类胆碱能药剂及治疗方法
公开(公告)号：US5482938A
公开(公告)日：1996-01-09
申请号：US189620
申请日：1994-02-01
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/46 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/28 , A61P43/00 , C07D205/06 , C07D207/22 , C07D211/72 , C07D223/06 , C07D225/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D451/10 , C07D453/02 , C07D471/08 , C07D487/08 , A61K31/535 , C07D413/00
CPC分类号： C07D487/08 , C07D211/72 , C07D451/04 , C07D453/02
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds are disclosed which are azabicyclo[2.2.2]oximes, azabicyclo[2.2.2]-amines, azabicyclo[3.2.1]oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms.
摘要翻译： 公开了含有有机氮的环状肟和胺取代的化合物，其是氮杂双环[2.2.2]肟，氮杂双环[2.2.2] - 胺，氮杂双环[3.2.1]肟和含胺杂环肟，其中杂环包含3 至7个碳原子。
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4.发明授权Oxime and amine substituted azabicyclo and azocyclo muscarinic agonists and methods of treatment 失效肟和胺取代的氮杂双环和偶氮环毒蕈碱激动剂和治疗方法
公开(公告)号：US5306718A
公开(公告)日：1994-04-26
申请号：US778412
申请日：1991-10-16
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/46 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/28 , A61P43/00 , C07D205/06 , C07D207/22 , C07D211/72 , C07D223/06 , C07D225/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D451/10 , C07D453/02 , C07D471/08 , C07D487/08 , A61K31/00
CPC分类号： C07D487/08 , C07D211/72 , C07D451/04 , C07D453/02
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds of the following general Formulas I, II and III are disclosed: ##STR1## Specifically the compounds are azabicyclo [2.2.1] omimes, azabicyclo [2.2.2] oximes, azabicyclo [2.2.1] amines, azabicyclo [2.2.2] amines, azabicyclo [3.2.1] oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 4 to 5 [3 to 7] carbon atoms.
摘要翻译： 公开了以下通式I，II和III的药用有用的含氮环状肟和胺取代的化合物：（*化学结构*）Ia（*化学结构*）IIb（*化学结构*）IIIc（*化学结构*） IVd具体地，化合物是氮杂双环（2.2.1），次氮杂双环（2.2.2）肟，氮杂双环（2.2.1）胺，氮杂双环（2.2.2）胺，氮杂双环（3.2.1）肟和含胺杂环肟，其中 该杂环含有4至5个（3至7个）碳原子。
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5.发明授权Azabicyclo and azacyclo oxime and amine cholinergic agents and methods of treatment 失效氮杂双环和吖嗪肟和胺类胆碱能药剂及治疗方法
公开(公告)号：US5346911A
公开(公告)日：1994-09-13
申请号：US110904
申请日：1993-08-24
申请人： Corinne E. Augelli-Szafran , Stephen D. Barrett , Bradley W. Caprathe , Adam A. Galan , Juan C. Jaen , David J. Lauffer , Walter H. Moos , Michael R. Pavia , Kathryn B. Sanders , Haile Tecle , Anthony J. Thomas
发明人： Corinne E. Augelli-Szafran , Stephen D. Barrett , Bradley W. Caprathe , Adam A. Galan , Juan C. Jaen , David J. Lauffer , Walter H. Moos , Michael R. Pavia , Kathryn B. Sanders , Haile Tecle , Anthony J. Thomas
IPC分类号： C07D211/72 , C07D451/04 , C07D453/02 , C07D487/08 , A61K31/44 , C07D211/70
CPC分类号： C07D211/72 , C07D451/04 , C07D453/02 , C07D487/08
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds which are azabicyclo[2.2.1]oximes, azabicyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes, and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms are disclosed.
摘要翻译： 含有偶氮二环[2.2.1]肟，氮杂双环[2.2.2]肟，氮杂双环[2.2.1]胺，氮杂双环[2.2.2]胺，氮杂双环[3.2.1] 肟和含有杂环肟的胺，其中杂环含有3至7个碳原子。
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公开(公告)号：US06511966B2
公开(公告)日：2003-01-28
申请号：US09933911
申请日：2001-08-20
IPC分类号： A01N4304
CPC分类号： A61K31/155 , A61K31/00 , A61K31/05 , A61K31/06 , A61K31/136 , C07C39/08 , C07C39/11 , C07C39/19 , C07C69/017 , C07C215/78 , C07C215/80 , C07C217/84 , C07C279/18 , C07D215/20 , C07D311/72
摘要： The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus. Parkinson's Disease, neuronal and cardiac ischemia. Huntington's disease and stroke.
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公开(公告)号：US4755594A
公开(公告)日：1988-07-05
申请号：US936766
申请日：1986-12-09
IPC分类号： C07H19/16 , A61K31/70 , C07H19/167
CPC分类号： C07H19/16
摘要： The present inventions are novel N.sup.6 -substituted adenosines wherein the N substituent is ##STR1## wherein Ar is an unsubstituted or substituted (1) phenyl, (2) 1- or 2-naphthalenyl, (3) 2- or 3-thienyl, (4) 2- or 3-furanyl, (5) 2-, 4-, or 5-thiazyl, (6) 2-, 3-, or 4-pyridyl, or (7) 2-pyrimidyl wherein the substituents include at least one of lower alkyl, halo, trifluoromethyl, hydroxy, lower alkoxy, lower acyloxyamino, N-lower monoalkyl or N,N-lower dialkylamino, lower thioalkyl, lower alkylsulfonyl, or nitro and R' is hydrogen or alkyl, A is ##STR2## wherein q, q', or q" are one to four, n and m are independently zero to three provided if A is a bond then n and m is at least 2 and if A is other than a bond then n and m is at least one. These novel adenosines have highly desirable central nervous system and cardiovascular activities and therefore the present invention also includes pharmaceutical compositions and methods of use therefor.
摘要翻译： 本发明是新的N6取代的腺苷，其中N取代基是其中Ar是未取代或取代的（1）苯基，（2）1-或2-萘基，（3）2-或3-噻吩基（ 4）2-或3-呋喃基，（5）2-，4-或5-噻唑基，（6）2-，3-或4-吡啶基或（7）2-嘧啶基，其中取代基至少包括 低级烷基，卤素，三氟甲基，羟基，低级烷氧基，低级酰氧基氨基，N-低级单烷基或N，N-低级二烷基氨基，低级硫代烷基，低级烷基磺酰基或硝基，R'是氢或烷基，A是< 其中q，q'或q“为1至4，n和m独立地为0至3，条件是如果A是键，则n和m至少为2，如果A不是键，则n和m是 最后一个。 这些新颖的腺苷具有非常需要的中枢神经系统和心血管活性，因此本发明还包括药物组合物及其用途的方法。
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8.发明授权公开(公告)号：US06498191B2
公开(公告)日：2002-12-24
申请号：US09733271
申请日：2000-12-07
IPC分类号： A61K31225
CPC分类号： A61K31/155 , A61K31/00 , A61K31/05 , A61K31/06 , A61K31/136 , C07C39/08 , C07C39/11 , C07C39/19 , C07C69/017 , C07C215/78 , C07C215/80 , C07C217/84 , C07C279/18 , C07D215/20 , C07D311/72
摘要： The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.
摘要翻译： 本发明一般涉及用于治疗线粒体功能障碍导致组织变性的线粒体保护剂，更具体地涉及与其相关的化合物，组合物和方法。 本发明的方法涉及向有需要的温血动物施用药学有效量的线粒体保护剂，本发明的组合物含有与药学上可接受的载体或稀释剂组合的线粒体保护剂。 可以通过本发明治疗的线粒体相关疾病包括（但不限于）阿尔茨海默氏病，糖尿病，帕金森病，神经元和心脏缺血，亨廷顿病和中风。
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公开(公告)号：US5536853A
公开(公告)日：1996-07-16
申请号：US225758
申请日：1994-04-11
申请人： David C. Spellmeyer , Walter H. Moos , Eric J. Martin , Ronald N. Zuckermann , Gregory Stauber , Kevin R. Shoemaker , Dane Goff
发明人： David C. Spellmeyer , Walter H. Moos , Eric J. Martin , Ronald N. Zuckermann , Gregory Stauber , Kevin R. Shoemaker , Dane Goff
IPC分类号： A61K38/00 , C07K5/083 , C07D317/50 , C07D317/54 , C07D317/58 , C07D319/14
CPC分类号： C07K5/0806 , A61K38/00
摘要： Compounds of Formula 1 bind opioid receptors: ##STR1## wherein X and Y are each independently ##STR2##
摘要翻译： 式1的化合物结合阿片受体：其中X和Y各自独立地为“IMAGE”
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公开(公告)号：US5447916A
公开(公告)日：1995-09-05
申请号：US99908
申请日：1993-07-30
IPC分类号： C07C237/22 , C07K5/02 , C07K5/023 , C07K5/083 , G01N33/566 , G01N33/74 , G01N33/94 , A61K38/05 , A61K38/06
CPC分类号： C07C237/22 , C07K5/0202 , C07K5/0806 , G01N33/566 , G01N33/74 , G01N33/9433 , Y10S514/821 , Y10S514/824 , Y10S514/913
摘要： Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.
摘要翻译： 下式的化合物：
可用于治疗由α1-肾上腺素能受体调节的病症。
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