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1.COMPOUNDS, THEIR SYNTHESES, COMPOSITIONS, AND METHODS TO TREAT CANCER 审中-公开
Title translation: 化合物,它们的合成,组合物和方法来治疗癌症公开(公告)号:WO2010093615A3
公开(公告)日:2010-11-25
申请号:PCT/US2010023604
申请日:2010-02-09
Applicant: TULANE UNIVERSITY , XAVIER UNIVERSITY OF LOUISIANA , BECKMAN BARBARA S , FOROOZESH MARYAM , LIU JIAWANG
Inventor: BECKMAN BARBARA S , FOROOZESH MARYAM , LIU JIAWANG
IPC: C07C235/02 , A61K31/133 , A61K31/16 , A61P35/00 , C07C215/34
CPC classification number: C07C233/60 , C07C215/24 , C07C233/21 , C07C237/06 , C07C251/24
Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
Abstract translation: 本文公开了化合物及其合成。 还描述了包含化合物的组合物和药物组合物,并且包括也包含脂质体的组合物。 还描述了用于治疗动物中癌症的方法,其包括施用化合物或包含化合物的组合物。
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公开(公告)号:WO2006117339A1
公开(公告)日:2006-11-09
申请号:PCT/EP2006/061917
申请日:2006-04-28
Applicant: SIKA TECHNOLOGY AG , GERBER, Ulrich
Inventor: GERBER, Ulrich
IPC: C08G14/06 , C07C215/34 , C08L63/00 , C08L75/00
CPC classification number: C08G14/06 , C07C215/34 , C08G18/3237 , C08G59/623 , C08G2190/00 , C09J163/00 , C09J175/12
Abstract: Die vorliegende Erfindung betrifft Mannichbasen, welche aus Resorcin, Formaldehyd, sowie Triethylentetramin und/oder Tetraethylenpentamin herstellbar sind. Weiterhin wird ein Verfahren zu deren Herstellung und deren Verwendung als Härter für Amin-reaktive Verbindungen offenbart. Besonders geeignet haben sich die Mannichbasen als Härterkomponente in Klebstoffen.
Abstract translation: 本发明涉及为Mannich其可以由间苯二酚,甲醛和三亚乙基四胺和/或四亚乙基五来制备碱。 此外,它们的制备和它们的用途的处理被公开为用于胺反应性化合物的固化剂。 的曼尼希碱作为固化在粘合剂组分已被证明特别适合的。
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公开(公告)号:WO02081078A3
公开(公告)日:2003-03-27
申请号:PCT/US0206367
申请日:2002-02-28
Applicant: 3M INNOVATIVE PROPERTIES CO
Inventor: RASMUSSEN JERALD K , KREPSKI LARRY R
IPC: B01J19/00 , C07B61/00 , C07C231/02 , C07C233/05 , C07C233/65 , C07K1/04 , C07C215/34 , C07C231/00 , C07C237/22 , C08F8/32
CPC classification number: C40B50/14 , B01J2219/00497 , B01J2219/005 , B01J2219/00527 , B01J2219/00596 , C07B2200/11 , C07H21/04 , C07K1/042
Abstract: Functionalized supports and methods for solid phase synthesis. Preferably, the functionalized support is azlactone-functionalized.
Abstract translation: 功能化支持和固相合成方法。 优选地,功能化载体是吖内酯官能化的。
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公开(公告)号:WO9964034A9
公开(公告)日:2000-06-29
申请号:PCT/US9911803
申请日:1999-06-07
Applicant: ADVANCED MEDICINE INC , GRIFFIN JOHN H , MORAN EDMUND J , CHOI SEOK KI
Inventor: GRIFFIN JOHN H , MORAN EDMUND J , CHOI SEOK-KI
IPC: G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00
CPC classification number: C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
Abstract: The present invention is directed to multibinding compounds which are beta 2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.
Abstract translation: 本发明涉及作为β2肾上腺素能受体激动剂的多重结合化合物,因此可用于治疗和预防呼吸系统疾病如哮喘,支气管炎等。 它们也可用于治疗神经系统损伤和早产。
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公开(公告)号:WO99064053A1
公开(公告)日:1999-12-16
申请号:PCT/US1999/012907
申请日:1999-06-08
IPC: G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00 , C07D317/10
CPC classification number: C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
Abstract: The present invention is directed to multibinding compounds which are beta 3-adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.
Abstract translation: 本发明涉及作为β3-肾上腺素能受体激动剂的多重结合化合物,因此可用于治疗和预防代谢性疾病如肥胖症,糖尿病等。
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6.
公开(公告)号:WO99064052A1
公开(公告)日:1999-12-16
申请号:PCT/US1999/012876
申请日:1999-06-08
IPC: G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00
CPC classification number: C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
Abstract: This invention relates to novel multibinding compounds that bind to leukotriene receptors and inhibit their activity. In particular, cysteinal leukotriene receptor antagonists and, most particularly leukotriene D4 receptor antagonist compounds are disclosed. The compounds of this invention comprise 2-10 leukotriene receptor ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to leukotriene receptors. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to the leukotriene receptors. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by leukotriene receptors. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.
Abstract translation: 本发明涉及结合白三烯受体并抑制其活性的新型多结合化合物。 特别地,公开了半胱氨酸白三烯受体拮抗剂,特别是白细胞三烯D4受体拮抗剂化合物。 本发明的化合物包含通过接头或接头共价连接的2-10个白三烯受体配体,其中其单价(即未连接)状态的配体结合白三烯受体。 将配体连接在一起的方式是这样形成的多结合剂与可用于结合白细胞三烯受体的相同数量的未连接的配体相比,显示增加的生物学和/或治疗效果。 本发明还涉及使用这些化合物的方法及其制备方法。 本发明的化合物特别可用于治疗由白细胞三烯受体介导的哺乳动物的疾病和病症。 因此,本发明还涉及包含药学上可接受的赋形剂和有效量的本发明化合物的药物组合物。
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7.COMPOUNDS, THEIR SYNTHESES, COMPOSITIONS, AND METHODS TO TREAT CANCER 审中-公开
Title translation: 化合物,其合成物,组合物和治疗癌症的方法公开(公告)号:WO2010093615A2
公开(公告)日:2010-08-19
申请号:PCT/US2010/023604
申请日:2010-02-09
Applicant: TULANE UNIVERSITY , XAVIER UNIVERSITY OF LOUISIANA , BECKMAN, Barbara, S. , FOROOZESH, Maryam , LIU, Jiawang
Inventor: BECKMAN, Barbara, S. , FOROOZESH, Maryam , LIU, Jiawang
IPC: C07C235/02 , C07C215/34 , A61K31/16 , A61K31/133 , A61P35/00
CPC classification number: C07C233/60 , C07C215/24 , C07C233/21 , C07C237/06 , C07C251/24
Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
Abstract translation: 本文公开了化合物及其合成。 还描述了包含化合物的组合物和药物组合物,并且包括还包含脂质体的组合物。 还描述了用于治疗动物中癌症的方法,包括给予化合物或包含化合物的组合物。
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公开(公告)号:WO9964041A9
公开(公告)日:2001-05-31
申请号:PCT/US9912727
申请日:1999-06-07
Applicant: ADVANCED MEDICINE INC , THOMAS G ROGER , JENKINS THOMAS E , GRIFFIN JOHN H
Inventor: THOMAS G ROGER , JENKINS THOMAS E , GRIFFIN JOHN H
IPC: G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00
CPC classification number: C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
Abstract: Disclosed are novel multi-binding compounds (agents) which bind to NMDA receptors. The compounds of this invention comprise a plurality of ligands each of which can bind to such receptors, thereby modulating the biological processes and/or functions thereof. Each of the ligands is covalently attached to a linker or linkers which may be the same or different to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation of the biological processes mediated by the NMDA receptor.
Abstract translation: 公开了结合NMDA受体的新型多重结合化合物(试剂)。 本发明的化合物包含多个配体,每个配体可以与这些受体结合,从而调节其生物学过程和/或功能。 每个配体共价连接到可以相同或不同以提供多结合化合物的连接体或连接体。 选择接头使得如此构建的多重结合化合物表现出由NMDA受体介导的生物过程的增加的调节。
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9.METHOD FOR PREPARING 2-2[(4-ALKYLPHENYL)-ETHYL]-2-AMINO-PROPANEDIOL AND INTERMEDIATES USEFUL IN SUCH PREPARATION 审中-公开
Title translation: 制备2-2 [(4-甲基苯基) - 乙基] -2-氨基 - 丙酰胺的方法和在制备中有用的中间体公开(公告)号:WO00053569A1
公开(公告)日:2000-09-14
申请号:PCT/CN2000/000046
申请日:2000-03-10
IPC: C07C215/28 , C07C213/00 , C07C215/34 , C07C231/08 , C07C231/14 , C07C233/22 , C07C233/31
CPC classification number: C07C215/28
Abstract: This invention relates to a method for preparing 2-2[(4-alkylphenyl)-ethyl]-2-amino-propanediol compounds of general formula (I), wherein R is C1-10 alkyl, preferably n-octyl, which comprises the following steps: reacting alkylbenzene (II) with acetyl chloride in the presence of Lewis acid; preparing p-alkyl alpha -halophenylethyl ketone (IV) according to a conventional method in the presence of a small amount of Lewis acid; condensing the obtained compound (IV) with 2-acylamino-malonate to give 2-acylamino-2-[2-p-alkylphenyl-2-oxo-ethyl]-malonate (VI) in the presence of a base; reducing product (VI) to 2-acylamino-2-[2-p-alkylphenyl-2-hydroxy-ethyl]-propanediol (VII); then hydrolyzing and hydrogenating compound (VII) to form compound (I). This invention also relates to the intermediates involved in the above method.
Abstract translation: 本发明涉及制备通式(I)的2-2 [(4-烷基苯基) - 乙基] -2-氨基 - 丙二醇化合物的方法,其中R是C 1-10烷基,优选正辛基,其包括 以下步骤:在路易斯酸存在下使烷基苯(II)与乙酰氯反应; 在少量路易斯酸存在下,按照常规方法制备对 - 烷基α-卤代苯乙基酮(Ⅳ); 将得到的化合物(Ⅳ)与2-酰基氨基丙二酸酯缩合,得到2-酰基氨基-2- [2-对烷基苯基-2-氧代 - 乙基] - 丙二酸二(VI) 将还原产物(VI)还原成2-酰基氨基-2- [2-对 - 烷基苯基-2-羟基 - 乙基] - 丙二醇(VII); 然后水解和氢化化合物(VII)以形成化合物(I)。 本发明还涉及上述方法中涉及的中间体。
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公开(公告)号:WO9964035A9
公开(公告)日:2000-07-06
申请号:PCT/US9911804
申请日:1999-06-07
Applicant: ADVANCED MEDICINE INC , GRIFFIN JOHN H , MORAN EDMUND J , CHOI SEOK KI
Inventor: GRIFFIN JOHN H , MORAN EDMUND J , CHOI SEOK-KI
IPC: G01N33/50 , A61K31/13 , A61K31/136 , A61K31/137 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/27 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/4164 , A61K31/4178 , A61K31/4184 , A61K31/435 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/55 , A61K31/551 , A61K31/5517 , A61K31/662 , A61K38/00 , A61K45/00 , A61K47/48 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/08 , A61P15/06 , A61P17/04 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P43/00 , C07B61/00 , C07C211/00 , C07C213/00 , C07C215/00 , C07C215/34 , C07C215/60 , C07C217/00 , C07C217/08 , C07C217/10 , C07C217/48 , C07C217/58 , C07C217/90 , C07C237/08 , C07C271/12 , C07C311/37 , C07C323/44 , C07C323/62 , C07D207/06 , C07D207/08 , C07D207/26 , C07D209/08 , C07D211/14 , C07D211/18 , C07D211/42 , C07D211/52 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/84 , C07D213/30 , C07D213/38 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/80 , C07D215/22 , C07D215/48 , C07D221/26 , C07D221/28 , C07D223/04 , C07D235/18 , C07D235/30 , C07D239/95 , C07D241/44 , C07D249/12 , C07D257/04 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D295/02 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/02 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D495/04 , C07D519/00 , C07K1/04 , C07K2/00 , C07K4/00 , C07K7/14 , C07K16/28 , C40B20/00 , G01N33/15 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/94 , G01N37/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K51/00
CPC classification number: C07D213/74 , A61K47/55 , C07B2200/11 , C07C215/60 , C07C217/08 , C07C323/62 , C07D211/42 , C07D211/56 , C07D213/80 , C07D263/32 , C07D263/34 , C07D265/32 , C07D277/24 , C07D277/28 , C07D277/34 , C07D401/12 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/12 , C07K1/047 , C40B40/00 , G01N33/9406 , G01N2333/62 , G01N2333/70578 , G01N2333/726 , G01N2500/00
Abstract: Disclosed are multibinding compounds which are beta 2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract translation: 公开了作为β2-肾上腺素能受体激动剂的多重联结化合物,并且可用于治疗和预防呼吸系统疾病如哮喘,支气管炎。 它们也可用于治疗神经系统损伤和早产。
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