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公开(公告)号：US4287341A
公开(公告)日：1981-09-01
申请号：US126838
申请日：1980-03-03
IPC分类号： C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20 , C07D401/04 , C07D403/04 , C07D413/04
CPC分类号： C07D413/04 , C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20
摘要： 2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.
摘要翻译： 式（I）的2,4-二氨基喹唑啉其中Y1是氢或氯，Y2是OR，Y3是氢或OR，使得当Y1是氢时，Y3是OR，当Y1是氯时，Y3是氢或 或其药学上可接受的盐; R表示具有1至3个碳原子的烷基; 单独取代，R 1和R 2各自为氢，具有1至5个碳原子的烷基，具有3至8个碳原子的环烷基，各自具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基 当与其连接的氮原子一起时，R 1和R 2形成任选地含有氧原子，硫或第二氮原子作为环成员的取代或未取代的杂环基; 它们用作抗高血压剂，含有它们的药物组合物和用于其生产的中间体。
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公开(公告)号：US4377581A
公开(公告)日：1983-03-22
申请号：US253052
申请日：1981-04-10
IPC分类号： C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20 , C07D413/04 , A61K31/505 , C07D403/04
CPC分类号： C07D413/04 , C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20
摘要： 2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such than when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.
摘要翻译： 式（I）的2,4-二氨基喹唑啉其中Y1是氢或氯，Y2是OR，Y3是氢或OR，例如当Y1是氢时，Y3是OR，当Y1是氯时，Y3是氢或 或其药学上可接受的盐; R表示具有1至3个碳原子的烷基; 单独取代，R 1和R 2各自为氢，具有1至5个碳原子的烷基，具有3至8个碳原子的环烷基，各自具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基 当与其连接的氮原子一起时，R 1和R 2形成任选地含有氧原子，硫或第二氮原子作为环成员的取代或未取代的杂环基; 它们用作抗高血压剂，含有它们的药物组合物和用于其生产的中间体。
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公开(公告)号：US4351940A
公开(公告)日：1982-09-28
申请号：US253236
申请日：1981-04-13
IPC分类号： C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20 , C07D413/04
CPC分类号： C07D413/04 , C07C205/44 , C07C205/59 , C07D211/18 , C07D211/32 , C07D211/42 , C07D211/46 , C07D239/95 , C07D239/96 , C07D267/10 , C07D307/68 , C07D319/20
摘要： 2,4-Diaminoquinazolines of the formula ##STR1## wherein Y.sup.1 is hydrogen or chloro, Y.sup.2 is OR, Y.sup.3 is hydrogen or OR such that when Y.sup.1 is hydrogen, Y.sup.3 is OR and when Y.sup.1 is chloro, Y.sup.3 is hydrogen or OR, and the pharmaceutically acceptable salts thereof; R represents an alkyl group having from one to three carbon atoms;taken separately, R.sup.1 and R.sup.2 are each hydrogen, alkyl having from one to five carbon atoms, cycloalkyl having from three to eight carbon atoms, alkenyl or alkynyl each having from three to five carbon atoms or hydroxy substituted alkyl having from two to five carbon atoms, when taken together with the nitrogen atom to which they are attached R.sup.1 and R.sup.2 form a substituted or unsubstituted heterocyclic group optionally containing an atom of oxygen, sulfur or a second atom of nitrogen as a ring member; their use as antihypertensive agents, pharmaceutical compositions containing them and intermediates for their production.
摘要翻译： 式（I）的2,4-二氨基喹唑啉其中Y1是氢或氯，Y2是OR，Y3是氢或OR，使得当Y1是氢时，Y3是OR，当Y1是氯时，Y3是氢或 或其药学上可接受的盐; R表示具有1至3个碳原子的烷基; 单独取代，R 1和R 2各自为氢，具有1至5个碳原子的烷基，具有3至8个碳原子的环烷基，各自具有3至5个碳原子的烯基或炔基或具有2至5个碳原子的羟基取代的烷基 当与其连接的氮原子一起时，R 1和R 2形成任选地含有氧原子，硫或第二氮原子作为环成员的取代或未取代的杂环基; 它们用作抗高血压剂，含有它们的药物组合物和用于其生产的中间体。
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公开(公告)号：US06503481B1
公开(公告)日：2003-01-07
申请号：US09561648
申请日：2000-05-02
IPC分类号： A61M1100
CPC分类号： A61K9/0078 , A61K9/0073 , A61M15/02 , B05B5/0255
摘要： A composition used in combination with an electrohydrodynamic device capable of delivering an active ingredient to the aerodigestive system of the user. The composition comprises three or optionally four basic components: an active ingredient; a carrier material in which the active ingredient may be dissolved, suspended, or emulsified; an aerosol properties adjusting material which provides the composition with the physical characteristics required to create an aerosol cloud by electrostatic or electrohydrodynamic means; and optionally at least one excipient that further adjusts, preserves, stabilizes, or enhances the overall performance of the composition.
摘要翻译： 与能够将活性成分输送到使用者的消气系统的电动液压装置组合使用的组合物。 组合物包含三种或任选的四种碱性组分：活性成分; 可以将活性成分溶解，悬浮或乳化的载体材料; 气溶胶性质调节材料，其通过静电或电流动力学方式为组合物提供产生气溶胶云所需的物理特性; 和任选的至少一种赋形剂，其进一步调节，保持，稳定或增强组合物的整体性能。
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公开(公告)号：US06348209B2
公开(公告)日：2002-02-19
申请号：US09875680
申请日：2001-06-06
申请人： Michael E. Placke , Anthony R. Imondi , Michael J. Brooker , John E. Frye , Praful K. Shah , Douglas R. Flanagan, Jr. , Maureen D. Donovan
发明人： Michael E. Placke , Anthony R. Imondi , Michael J. Brooker , John E. Frye , Praful K. Shah , Douglas R. Flanagan, Jr. , Maureen D. Donovan
IPC分类号： A61F1300
CPC分类号： A61K9/0073 , A61K31/00
摘要： A formulation, method, and apparatus for treating neoplasms such as cancer by administering a pharmaceutically effective amount of highly toxic composition by inhalation, wherein the composition is a non-encapsulated antineoplastic drug.
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公开(公告)号：US20080145433A1
公开(公告)日：2008-06-19
申请号：US11935474
申请日：2007-11-06
CPC分类号： A61K31/505 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/2813 , A61K9/2853 , A61K9/2866
摘要： A solid discrete orally deliverable pharmaceutical dosage form comprises darusentan and one or more pharmaceutically acceptable excipients; wherein (a) the darusentan is in solid particulate form having a mean particle size of about 5 to about 200 μm and is present in the dosage form in an amount of about 1 to about 600 mg; and (b) the dosage form exhibits at least about 90% dissolution of the darusentan in 30 minutes in a standard in vitro dissolution test. A method for lowering blood pressure, for example in a patient having resistant hypertension, comprises administering such a dosage form once daily to the patient.
摘要翻译： 固体分散的口服递送药物剂型包含darusentan和一种或多种药学上可接受的赋形剂; 其中（a）所述darusentan是固体颗粒形式，其平均粒度为约5至约200μm，并且在剂型中以约1至约600mg的量存在; 和（b）在标准体外溶出试验中，剂型在30分钟内显示至少约90％的darusentan溶解。 一种降低血压的方法，例如在具有耐药性高血压的患者中，包括每天向患者施用这种剂型。
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公开(公告)号：US06451784B1
公开(公告)日：2002-09-17
申请号：US09517915
申请日：2000-03-03
IPC分类号： A01N5502
CPC分类号： A61K31/555 , A61K9/0073 , A61K31/00 , A61K31/66 , A61K2300/00
摘要： A formulation and method for treating neoplasms such as cancer by administering a pharmaceutically effective amount or carboplatin by inhalation.
摘要翻译： 通过吸入施用药物有效量或卡铂来治疗肿瘤如癌症的制剂和方法。
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