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![SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE SALTS](/abs-image/US/2014/03/13/US20140072529A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140072529A1
公开(公告)日：2014-03-13
申请号：US14009599
申请日：2012-03-29
IPC分类号： C07D487/04 , A61K45/06 , A61K31/5377
CPC分类号： A61K31/5377 , A61K45/06 , C07D487/04
摘要： The present invention relates:—to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo-[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II): or a tautomer, solvate or hydrate thereof;—to methods of preparing said dihydrochloride salt;—to said dihydrochloride salt for the treatment and/or prophylaxis of a disease;—to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer;—to a pharmaceutical composition comprising said dihydrochloride salt; and to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agents.
摘要翻译： 本发明涉及2-氨基-N-〔7-甲氧基-8-（3-吗啉-4-基丙氧基）-2,3-二氢咪唑并〔1,2-c〕喹唑啉-5-基〕嘧啶 式（II）的5-甲酰胺二盐酸盐：或其互变异构体，溶剂化物或水合物; - 制备所述二盐酸盐的方法; - 用于治疗和/或预防疾病的所述二盐酸盐; - 使用 的所述二盐酸盐用于制备用于治疗和/或预防疾病，特别是高增殖和/或血管生成障碍的药物，更特别是用于治疗或预防癌症，特别是肺癌， 特定的非小细胞肺癌，结肠直肠癌，黑素瘤，胰腺癌，肝细胞癌，胰腺癌，肝细胞癌或乳腺癌; - 包含所述二盐酸盐的药物组合物; 以及包含所述二盐酸盐与一种或多种其它药剂组合的药物组合。
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公开(公告)号：US08372972B2
公开(公告)日：2013-02-12
申请号：US13308418
申请日：2011-11-30
IPC分类号： C07D239/72
CPC分类号： C07D239/84 , C07D239/78 , C07D239/80
摘要： The present invention relates to a process for the preparation of dihydroquinazolines, for example, methyl (S)-{8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoro -methyl)-phenyl]-3,4-dihydroquinazolin-4-yl}acetate (2S,3S)-2,3-bis[(4-methylbenzoyl) -oxy]succinic acid salt, which are used for the production of antiviral medicaments.
摘要翻译： 本发明涉及制备二氢喹唑啉的方法，例如（S） - {8-氟-2- [4-（3-甲氧基苯基）哌嗪-1-基] -3- [2-甲氧基 - 5-（三氟甲基） - 苯基] -3,4-二氢喹唑啉-4-基}乙酸酯（2S，3S）-2,3-双[（4-甲基苯甲酰基） - 氧基]琥珀酸盐 生产抗病毒药物。
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公开(公告)号：US20120130072A1
公开(公告)日：2012-05-24
申请号：US13308418
申请日：2011-11-30
IPC分类号： C07D403/04
CPC分类号： C07D239/84 , C07D239/78 , C07D239/80
摘要： The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.
摘要翻译： 本发明涉及用于制备药物的二氢喹唑啉的制备方法。
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公开(公告)号：US20120129857A1
公开(公告)日：2012-05-24
申请号：US13291271
申请日：2011-11-08
申请人： Hans-Christian MILITZER , Jörg GRIES , Stefan KOEP
发明人： Hans-Christian MILITZER , Jörg GRIES , Stefan KOEP
IPC分类号： A61K31/5377 , A61P13/12 , A61P7/06 , C07D413/14 , A61P9/00
CPC分类号： C07D403/14 , A61K31/5377 , A61K45/06
摘要： The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1 H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
摘要翻译： 本申请涉及1- [6-（吗啉-4-基）嘧啶-4-基] -4-（1H-1,2,3-三唑-1-基）-1H-吡唑-5-基] 橄榄石，其制备方法，其用于治疗和/或预防疾病及其用于制备用于治疗和/或预防疾病，特别是心血管和血液病和肾脏疾病的药物的用途，以及 用于促进伤口愈合。
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公开(公告)号：US07847126B2
公开(公告)日：2010-12-07
申请号：US11810374
申请日：2007-06-05
CPC分类号： C07B37/04 , B01J31/24 , B01J31/2404 , B01J31/2409 , B01J31/2414 , B01J31/2447 , B01J2231/4211 , B01J2231/4233 , B01J2231/4238 , B01J2231/4255 , B01J2231/4261 , B01J2231/4266 , B01J2231/4283 , B01J2231/4288 , B01J2231/4294 , B01J2531/0205 , C07F9/5068 , C07F9/5442
摘要： The invention relates to a process for synthesizing tertiary phosphines by reacting halophosphines with organomagnesium compounds in the presence of copper compounds and optionally of salts.
摘要翻译： 本发明涉及在铜化合物和任选的盐存在下使卤代膦与有机镁化合物反应合成叔膦的方法。
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公开(公告)号：US20090221822A1
公开(公告)日：2009-09-03
申请号：US11922280
申请日：2006-06-02
IPC分类号： C07D403/04 , C07D239/74
CPC分类号： C07D239/84 , C07D239/78 , C07D239/80
摘要： The present invention relates to a process for the preparation of dihydroquinazolines, which are used for the production of medicaments.
摘要翻译： 本发明涉及用于制备药物的二氢喹唑啉的制备方法。
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公开(公告)号：US06403622B1
公开(公告)日：2002-06-11
申请号：US09806430
申请日：2001-04-27
申请人： Markus Heil , Hans-Christian Militzer , Thomas Bretschneider , Bernd Alig , Astrid Mauler-Machnik , Klaus Stenzel , Ulrike Wachendorff-Neumann
发明人： Markus Heil , Hans-Christian Militzer , Thomas Bretschneider , Bernd Alig , Astrid Mauler-Machnik , Klaus Stenzel , Ulrike Wachendorff-Neumann
IPC分类号： C07D41712
CPC分类号： A01N43/80 , A01N43/82 , C07D417/12
摘要： Novel phenylacetic acid heterocyclyl amides of the formula in which R1, R2, R3, R4, A, X and n are as defined in the description, a process for preparing these novel compounds and their use for controlling undesirable microorganisms and animal pests. Novel intermediates of the formula and a plurality of processes for their preparation.
摘要翻译： R1，R2，R3，R4，A，X和n的新型苯乙酸杂环基酰胺如说明书中所定义，制备这些新化合物的方法及其用于防治不期望的微生物和动物害虫的新型中间体 配方及其制备方法。
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公开(公告)号：US5935988A
公开(公告)日：1999-08-10
申请号：US679027
申请日：1996-07-12
申请人： Michael Matzke , Hans-Christian Militzer , Joachim Mittendorf , Franz Kunisch , Axel Schmidt , Wolfgang Schonfeld , Karl Ziegelbauer
发明人： Michael Matzke , Hans-Christian Militzer , Joachim Mittendorf , Franz Kunisch , Axel Schmidt , Wolfgang Schonfeld , Karl Ziegelbauer
IPC分类号： C07K5/00 , A61K31/195 , A61K31/27 , A61K38/05 , A61P31/04 , A61P31/10 , C07C229/48 , C07C231/02 , C07C237/04 , C07K5/023 , A61K31/40
CPC分类号： C07C237/04 , A61K31/195 , A61K38/05 , C07C229/48 , C07C2101/08
摘要： The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.
摘要翻译： 本发明涉及α-氨基酸和/或其衍生物和环戊烷-β-氨基酸和/或其衍生物的混合物，上述α-氨基酸的二肽和环戊烷-β-氨基酸以及上述混合物的混合物 和与纯环戊烷-β-氨基酸相比，在温血动物中具有改善的耐受性的二肽。
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公开(公告)号：US20130310381A1
公开(公告)日：2013-11-21
申请号：US13988141
申请日：2011-11-15
申请人： Hans-Christian Militzer , Jörg Gries , Stefan Koep
发明人： Hans-Christian Militzer , Jörg Gries , Stefan Koep
IPC分类号： C07D403/14 , A61K45/06 , A61K31/5377
CPC分类号： C07D403/14 , A61K31/5377 , A61K45/06
摘要： The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
摘要翻译： 本申请涉及1- [6-（吗啉-4-基）嘧啶-4-基] -4-（1H-1,2,3-三唑-1-基）-1H-吡唑-5-醇酸钠 ，其制备方法，其用于治疗和/或预防疾病及其用于制备用于治疗和/或预防疾病，特别是心血管和血液病和肾脏疾病的药物的用途，以及用于 促进伤口愈合。
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10.发明授权Polyamino acid-catalyzed process for the enantioselective epoxidation of α,β-unsaturated enones and α,β-unsaturated sulfones 失效用于α，β-不饱和烯酮和α，β-不饱和砜的对映选择性环氧化的聚氨基酸催化方法公开(公告)号：US07208447B2
公开(公告)日：2007-04-24
申请号：US10926458
申请日：2004-08-25
IPC分类号： B01J20/26 , C07D301/12 , C07D303/32 , C08L77/00
CPC分类号： C07D303/32 , C07B2200/07 , C07D303/48
摘要： The invention relates to a novel process that makes it possible to epoxidize α,β-unsaturated enones or α,β-unsaturated sulfones with high conversions and enantiomeric excesses in a two-phase system without addition of water in the presence of an organic solvent, a base, an oxidant, a diastereomer- and enantiomer-enriched homo-polyamino acid that has not been separately preactivated as catalyst, and a specific phase-transfer catalyst as cocatalyst.
摘要翻译： 本发明涉及一种新的方法，其可以在有机溶剂的存在下在不加水的情况下在两相体系中以高转化率和对映体过量进行环氧化的α，β-不饱和烯酮或α，β-不饱和砜， 没有单独预活化作为催化剂的碱，氧化剂，非对映异构体和对映体富集的均聚氨基酸，以及作为助催化剂的特定相转移催化剂。
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