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1. 发明授权

US5106840A Method of preparing n-oxo-tetrahydro-beta-carbolines 失效
标题翻译：制备N-氧代四氢 - 碳 - 碳的方法
公开(公告)号：US5106840A
公开(公告)日：1992-04-21
申请号：US533415
申请日：1990-06-05
申请人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
发明人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
IPC分类号： C07D209/14 , A61K31/435 , A61K31/535 , A61K31/55 , A61P31/12 , A61P35/00 , C07D498/14 , C07D499/14 , C07D515/14
CPC分类号： C07D515/14
摘要： The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.1, andA together with the group --C--N--O--, forms a saturated heterocyclic ring systems consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group, O, S and N may be present, which ring system may be substituted with one or more of the substituents alkyl, alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl-or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ring closure reaction of compounds of formula 2 ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a funciton during the ring closure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumor activity.

2. 发明授权

US5843948A Piperazinophenyl- and piperazinophenyloxycarboxylic acid derivatives, and processes and intermediates for their preparation and pharmaceutical compositions comprising them 失效
标题翻译：哌嗪基苯基和哌嗪苯氧基羧酸衍生物，以及其制备方法和中间体以及包含它们的药物组合物
公开(公告)号：US5843948A
公开(公告)日：1998-12-01
申请号：US994754
申请日：1997-12-19
申请人： Wolfgang Kehrbach , Uwe Schoen , Jack A. J. den Hartog , Jan H. van Maarseveen , Chris G. Kruse , Jochen Antel , Jan-Hendrik Reinders , Dieter Ziegler , Gerhard-Wilhelm Bielenberg
发明人： Wolfgang Kehrbach , Uwe Schoen , Jack A. J. den Hartog , Jan H. van Maarseveen , Chris G. Kruse , Jochen Antel , Jan-Hendrik Reinders , Dieter Ziegler , Gerhard-Wilhelm Bielenberg
IPC分类号： C07D295/08 , A61K31/495 , A61P7/02 , C07D213/74 , C07D213/78 , C07D295/14 , C07D295/155 , C07D295/135 , C07D401/04
CPC分类号： C07D213/74 , C07D295/155 , Y02P20/55
摘要： Compounds having fibrinogen receptor-antagonistic activity, of the general formula I ##STR1## in which Z is oxygen or a methylene group, B is a phenyl or pyridyl radical, R.sup.1 is hydrogen or a group forming a biolabile ester, and their physiologically acceptable acid addition salts and physiologically acceptable salts of acids of formula I.
摘要翻译：具有纤维蛋白原受体拮抗活性的化合物，其中Z为氧或亚甲基的通式I ，B为苯基或吡啶基，R 1为氢或形成不可生物酯的基团及其生理学上可接受的酸式I的酸的加成盐和生理上可接受的盐。

3. 发明授权

US5348949A Method of preparing N-oxo-tetrahydro-.beta.-carbolines 失效
标题翻译：制备N-氧代 - 四氢-β-咔啉的方法
公开(公告)号：US5348949A
公开(公告)日：1994-09-20
申请号：US16675
申请日：1993-02-12
申请人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
发明人： Peter H. H. Hermkens , Jan H. Van Maarseveen , Johan W. Scheeren , Cornelis G. Kruse
IPC分类号： C07D209/14 , A61K31/435 , A61K31/535 , A61K31/55 , A61P31/12 , A61P35/00 , C07D498/14 , C07D499/14 , C07D515/14 , C07D209/24
CPC分类号： C07D515/14
摘要： The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
摘要翻译：本发明涉及制备式I化合物的N-氧代 - 四氢-β-咔啉的方法。式（2）化合物的反应其中Z是醛官能团或缩醛官能团，或是一种官能团，可以在环形防腐反应过程中转化成这样的功能。具有式1的化合物组中的雌二醇衍生物具有强的抗病毒和抗肿瘤活性。

4. 发明授权

US07202238B2 Diazabicyclo alkane derivatives with NK1 antagonistic activity 有权
标题翻译：具有NK1拮抗活性的二氮杂双环烷烃衍生物
公开(公告)号：US07202238B2
公开(公告)日：2007-04-10
申请号：US10490364
申请日：2003-04-02
申请人： Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
发明人： Dirk de Boer , Hein K. A. C. Coolen , Mayke B. Hesselink , Wouter I. Iwema Bakker , Gijsbert D. Kuil , Jan H. van Maarseveen , Andrew C. McCreary , Gustaaf J. M. van Scharrenburg
IPC分类号： A01N43/00 , A01N43/58 , A01N43/50 , A61K31/55 , C07D241/36
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to a group of unique diazabicyclo alkane derivatives having interesting neurokinin-NK1 receptor antagonistic activity represented by the general formula (1) wherein: R1 represents phenyl, 2-indolyl, 3-indolyl, 3-indazolyl or benzo[b]thiophen-3-yl, which groups may be substituted with halogen or alkyl (1–3C), R2 and R3 independently represent halogen, H, OCH3, CH3 and CF3, R4, R5 and R6 independently represent H, OH, O-alkyl(1–4C), CH2OH, NH2, dialkyl(1–3C)N, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or morpholin-4-yl substituted with one or two methyl or methoxymethyl groups, morpholin-4-ylamino, morpholin-4-ylmethyl, imidazol-1-yl, thiomorpholin-4-yl, 1,1-dioxothiomorpholin-4-yl or 3-oxa-8-azabicyclo[3.2.1]oct-8-yl; R4 and R5 together may represent a keto, a 1,3-dioxan-2-yl or a 1,3-dioxolan-2-yl group, X represents either O or S, n has the value of 1, 2 or 3, a is the asymmetrical carbon atom 8a, 9a or 10a when n equals 1, 2 or 3 respectively The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions containing at least one of these compounds as an active ingredient
摘要翻译：本发明涉及具有由通式（1）表示的具有感兴趣的神经激肽NK 1受体拮抗作用的独特的二氮杂双环烷烃衍生物组，其中：R 1表示苯基， 2-吲哚基，3-吲哚基，3-吲唑基或苯并[b]噻吩-3-基，该基团可被卤素或烷基（1-3C），R 2和R 2 > 3个独立地表示卤素，H，OCH 3，CH 3和CF 3，R 4， >，R 5和R 6独立地表示H，OH，O-烷基（1-4C），CH 2 OH，NH （1-3C）N，吡咯烷-1-基，哌啶-1-基，吗啉-4-基或被一个或两个甲基或甲氧基甲基取代的吗啉-4-基，吗啉代 - 吡啶-4-基氨基，吗啉-4-基甲基，咪唑-1-基，硫代吗啉-4-基，1,1-二氧代硫代吗啉-4-基或3-氧杂-8-氮杂双环[3.2.1]辛-8-基; R 4和R 5一起可以表示酮基，1,3-二氧杂环戊烷-2-基或1,3-二氧戊环-2-基，X表示 O或S，n的值为1,2或3，当n分别为1,2或3时，a为非对称碳原子8a，9a或10a。本发明还涉及一种制备新化合物的方法以及含有这些化合物中的至少一种作为活性成分的药物组合物

5. 发明授权

US07094779B2 Piperazine oxime dervatives having NK-1 receptor antagonistic activity 有权
标题翻译：具有NK-1受体拮抗活性的哌嗪肟衍生物
公开(公告)号：US07094779B2
公开(公告)日：2006-08-22
申请号：US10480542
申请日：2002-07-03
申请人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
发明人： Wouter I. Iwema Bakker , Jan H. van Maarseveen , Hein K. A. C. Coolen , Martinus Th. M. Tulp , Arnoldus H. J. Herremans , Andrew C. Mccreary , Gustaaf J. M. van Scharrenburg , Adrianus van den Hoogenband
IPC分类号： A61K31/496 , C07D403/06 , C07D413/14 , C07D471/04
CPC分类号： C07D401/14 , C07D241/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/06 , C07D471/04
摘要： The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein: X represents phenyl or pyridyl substituted with 1 or 2 substituents from the group CH3, CF3, OCH3, halogen, cyano and 5-CF3-tetrazol-1-yl; Y represents 2- or 3-indolyl, phenyl, 7-aza-indol-3-yl or 3-indazolyl, 2-naphthyl, 3-benzo[b]thiophenyl, 2-benzofuranyl, which groups may be substituted with one or more halogen or alkyl (1–3C); n has the value 0–3; m has the value 0–2; R1 represents NH2, NH-alkyl (1–3C), dialkyl (1–3C)N, morpholino or morpholino substituted with one or two methyl and/or methoxymethyl groups, thiomorpholino, 1,1-dioxothiomorpholino, 2-, 3- or 4-pyridyl or 4-CH3-piperazinyl; R2 is hydrogen, alkyl (1–4C) or phenyl, or R2 together with (CH2)m wherein m is 1, and the intermediate carbon, nitrogen and oxygen atoms forms an isoxazolyl or a 4,5-dihydroisoxazolyl group; R3 and R4 independently represent hydrogen or methyl, or R3 and R4 together are oxygen. The invention also relates to a method for the preparation of the novel compounds, and to pharmaceutical compositions comprising compounds with formula (1) as an active ingredient and the use of these compounds for the treatment of disorders in which neurokinin-1 receptors are involved
摘要翻译：本发明涉及一组具有有趣的NK-1拮抗活性的新型哌嗪肟衍生物。本发明涉及通式（1）的化合物，其中：X表示苯基或被1或2个取代基取代的吡啶基，其中CH 3，CF 3，OCH 3， N 3，卤素，氰基和5-CF 3 - 四唑-1-基; Y代表2-或3-吲哚基，苯基，7-氮杂 - 吲哚-3-基或3-吲唑基，2-萘基，3-苯并[b]噻吩基，2-苯并呋喃基，它们可以被一个或多个卤素或烷基（1-3C）; n的值为0-3; m的值为0-2; R 1表示NH 2，NH-烷基（1-3C），（1-3C）二烷基，吗啉代或吗啉基，被一或两个甲基和/或甲氧基甲基基团，硫代吗啉代，1,1-二氧代硫代吗啉代，2-，3-或4-吡啶基或4- CH 3 - 哌嗪基; R 2是氢，烷基（1-4C）或苯基，或R 2和（CH 2 CH 2）m，其中m为1，中间碳，氮和氧原子形成异恶唑基或4,5-二氢异恶唑基; R 3和R 4独立地代表氢或甲基，或R 3和R 4一起是氧。本发明还涉及一种制备新化合物的方法，以及包含式（1）化合物作为活性成分的药物组合物，以及这些化合物用于治疗涉及神经激肽-1受体的疾病的用途

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