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1. 发明公开

EP2439203A1 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译： Arylsulfonylmethyl-或芳基磺酰胺取代的芳族化合物用于治疗疾病有关多巴胺D 3受体的调节治疗
公开(公告)号：EP2439203A1
公开(公告)日：2012-04-11
申请号：EP12150319.7
申请日：2005-10-14
申请人： Abbott GmbH & Co. KG
发明人： Drescher, Karla , Haupt, Andreas , Unger, Liliane , Turner, Sean, Colm , Braje, Wilfried , Grandel, Roland , Henry, Christophe
IPC分类号： C07D311/04 , C07D215/38 , C07C211/19 , A61K31/13 , A61K31/47 , A61K31/35 , A61P25/16 , C07C311/21 , C07C311/29 , C07C311/44 , C07D207/10 , C07D211/10 , C07D239/84 , C07D263/32 , C07D277/82 , C07D413/04 , C07D491/04
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula I

wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R a and wherein Ar may also carry 1 or 2 radicals R b ;
X is N or CH;
Y is O, S, -CH=N-, -CH=CH- or -N=CH-;
A is CH 2 , O or S;
E is CR 6 R 7 or NR 3 ;
R 1 is C 1 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -cycloalkylmethyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -cycloalkylmethyl, fluorinated C 3 -C 4 -alkenyl, formyl or C 1 -C 3 -alkylcarbonyl;
R 1a is H, C 2 -C 4 -alkyl, C 3 -C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, or R 1a and R 2 together are (CH 2 ) n with n being 2 or 3, or R 1a and R 2a together are (CH 2 ) n with n being 2 or 3;
R 2 and R 2a are independently of each other H, CH 3 , CH 2 F, CHF 2 or CF 3 ;
R 3 is H or C 1 -C 4 -alkyl;
R 6 , R 7 independently of each other are selected from H, C 1 -C 2 -alkyl and fluorinated C 1 -C 2 -alkyl;
and the physiologically tolerated acid addition salts thereof.
The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

2. 发明公开

EP1812416A1 ARYLSULFONYLMETHYL OR ARYLSULFONAMIDE SUBSTITUTED AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MADULATION OF THE DOPAMINE D3 RECEPTOR 有权
标题翻译： ARYLSULFONYLMETHYL- OR芳基磺酰胺取代的芳族化合物，其治疗疾病都适合于多巴胺D3受体反应的调制
公开(公告)号：EP1812416A1
公开(公告)日：2007-08-01
申请号：EP05800649.5
申请日：2005-10-14
申请人： Abbott GmbH & Co. KG
发明人： DRESCHER, Karla , HAUPT, Andreas , UNGER, Liliane , TURNER, Sean, C. , BRAJE, Wilfried , GRANDEL, Roland , HENRY, Christophe
IPC分类号： C07D311/04 , C07D215/38 , C07C211/19 , A61K31/13 , A61K31/47 , A61K31/35 , A61P25/16
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04
摘要： The present invention relates to aromatic compounds of the formula (I), wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, -CH=N-, -CH=CH- or -N=CH-; A is CH2i O or S; E is CR6R7 or NR 3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C,-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4 -cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

3. 发明公开

EP1550648A1 Verfahren zur Herstellung von TCD-Diamin 审中-公开
公开(公告)号：EP1550648A1
公开(公告)日：2005-07-06
申请号：EP04025482.3
申请日：2004-10-27
申请人： Celanese Chemicals Europe GmbH
发明人： Lappe, Peter, Dr. , Springer, Helmut , Lukas, Rainer, Dr.
IPC分类号： C07C209/26 , C07C211/19 , C07C45/50 , C07C47/347 , C07C47/445
CPC分类号： C07C209/26 , C07C47/347 , C07C47/445 , C07C2603/68 , C07C211/19
摘要： Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung von 3(4),8(9)-Bis(aminomethyl)-tricyclo[5.2.1.0 2.6 ]decan durch Hydroformylierung von Dicyclopentadien mit nachfolgender reduktiver Aminierung. Die Hydroformylierung von Dicyclopentadien wird in zwei Stufen durchgeführt, wobei in einer ersten Hydroformylierungsstufe die Umsetzung in einem heterogenen Reaktionssystem unter Verwendung einer wässrigen Lösung, wasserlösliche organische Phosphor(III)verbindungen in komplexer Bindung enthaltender Übergangsmetallverbindungen der Gruppe VIII des Periodensystems zum 8(9)-Formyl-tricyclo[5.2.1.0 2.6 ]dec-3-en erfolgt und wobei in einer zweiten Hydroformylierungsstufe das so erhaltene 8(9)-Formyl-tricyclo[5.2.1.0 2.6 ]dec-3-en in homogener organischer Phase in Gegenwart von Übergangsmetallverbindungen der Gruppe VIII des Periodensystems der Elemente in 3(4),8(9)-Bisformyl-tricyclo[5.2.1.0 2.6 ]decan überführt wird.
摘要翻译：制备3（4），8（9） - 双（氨甲基）三环 - [5.2.1.0（2,6）]癸烷包括在第一加氢甲酰化阶段使二环戊二烯与合成气反应，得到8（9） - 甲酰基 - 三环[ 5.2.1.0（2,6）]癸-3-烯（a）; 从水相中分离有机相; 在第二加氢甲酰化阶段使（a）与合成气反应形成3（4），8（9） - 二甲基三环 - [5.2.-1.0（2,6）]癸烷（b）并进行厌食。制备3（4），8（9） - 双（氨基甲基）三环 - [5.2.1.0（2,6）]癸烷（TCD-二胺）包括在非均相反应体系中的第一加氢甲酰化阶段使二环戊二烯与合成气反应，过渡金属化合物的水溶液，其含有复合结合形式的水溶性有机磷（III）化合物，第Ⅷ组，70-150℃，压力为0.5-10MPa，得到8（9） - 甲酰三环[5.2.1.0（2,6）]癸-3-烯（a）; 从水相中分离有机相; 在（a）与合成气反应形成3（4），8（9） - 双甲基三环[5.2.-1.0（2,6）]癸烷（b），在均相有机相的第二加氢甲酰化阶段的第VIII族过渡金属化合物在70-140℃和5-35MPa的压力下进行; 并进行厌食。

4. 发明公开

EP0870757A3 Fluoro-substituted adamantane derivatives 失效
标题翻译： Fluorosubstituierte金刚烷衍生物
公开(公告)号：EP0870757A3
公开(公告)日：2000-06-07
申请号：EP98302196.5
申请日：1998-03-24
申请人： PFIZER INC.
发明人： Jasys, Vytautus John , Volkmann, Robert Alfred
IPC分类号： C07C211/38 , C07C211/19 , C07C61/15 , C07C69/753 , C07C233/58 , A61K31/13 , A61K31/16 , A61K31/19
CPC分类号： C07C69/00 , C07C61/15 , C07C211/38 , C07C271/24 , C07C2603/00 , C07C2603/74
摘要： The invention relates to fluoro-substituted adamantane derivatives of the formula and to pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , and R 4 are as defined herein. The invention also relates to methods of treating neurological disorders, such as memory loss and Parkinson's disease, and bacterial and viral infections, through administration of a therapeutically effective amount of a compound of formula I. The invention also relates to a method of increasing the metabolic stability of an adamantane-containing pharmaceutical compound by incorporating a fluoro substituent on at least one bridge-head carbon of the adamantyl group of said adamantane-containing pharmaceutical compound.

5. 发明授权

EP2439203B1 Arylsulfonylmethyl or arylsulfonamide substituted aromatic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译： Arylsulfonylmethyl-或芳基磺酰胺取代的芳族化合物用于治疗疾病有关多巴胺D 3受体的调节治疗
公开(公告)号：EP2439203B1
公开(公告)日：2014-11-19
申请号：EP12150319.7
申请日：2005-10-14
申请人： AbbVie Deutschland GmbH & Co KG
发明人： Drescher, Karla , Haupt, Andreas , Unger, Liliane , Turner, Sean, Colm , Braje, Wilfried , Grandel, Roland , Henry, Christophe
IPC分类号： C07D311/04 , C07D215/38 , C07C211/19 , A61K31/13 , A61K31/47 , A61K31/35 , A61P25/16 , C07C311/21 , C07C311/29 , C07C311/44 , C07D207/10 , C07D211/10 , C07D239/84 , C07D263/32 , C07D277/82 , C07D413/04 , C07D491/04
CPC分类号： C07C311/21 , C07C311/29 , C07C311/44 , C07C2601/02 , C07C2602/10 , C07D207/10 , C07D211/10 , C07D215/38 , C07D239/84 , C07D263/32 , C07D277/82 , C07D311/04 , C07D413/04 , C07D491/04

6. 发明公开

EP2708527A4 ALDEHYDE COMPOUND PRODUCTION METHOD 有权
标题翻译：生产醛类化合物的方法
公开(公告)号：EP2708527A4
公开(公告)日：2014-09-24
申请号：EP12782970
申请日：2012-05-07
申请人： MITSUI CHEMICALS INC
发明人： KUMA SHIGETOSHI , SAKATA MICHIHARU , TOKUNAGA KOUICHI , SHIMAKAWA CHITOSHI , KAKINUMA NAOYUKI , FURUYA MASAYUKI , TANAKA MAMORU
IPC分类号： C07C45/49 , C07B61/00 , C07C45/29 , C07C47/347 , C07C209/26 , C07C209/48 , C07C209/52 , C07C211/19 , C07C253/30 , C07C255/47 , C07C263/10 , C07C265/14
CPC分类号： C07C253/30 , C07C45/29 , C07C45/49 , C07C209/26 , C07C209/48 , C07C209/52 , C07C263/10 , C07C2602/42 , C07C211/19 , C07C265/14 , C07C255/47 , C07C47/347
摘要： A process for producing an aldehyde compound of the invention comprising: reacting a compound represented by the following formula (a1) or (a2) with a hydrogen and a carbon monoxide in a presence of a compound containing a metal belonging to Groups 8 to 10 and a phosphorous compound so as to satisfy the following conditions (1) and (2) to synthesize an aldehyde compound; wherein the condition (1) is that a content of a metal included in the compound containing a metal belonging to Groups 8 to 10 is 0.01 ppmmol to 300 ppmmol with respect to 1 mol of the compound represented by the formula (a1) or (a2), and wherein the condition (2) is that a molar ratio represented by the phosphorous compound (mol)/ the metal (mol) is 100 or more;
摘要翻译：一种制备本发明的醛化合物的方法，包括：在含有属于第8〜10族的金属的化合物的存在下，使由下式（a1）或（a2）表示的化合物与氢气和一氧化碳反应，以及一种磷化合物，以满足以下条件（1）和（2）来合成醛化合物; 其中，条件（1）是含有属于第8〜10族的金属的化合物中含有的金属的含量相对于1摩尔式（a1）表示的化合物或（a2 ），其中条件（2）是由磷化合物（摩尔）/金属（摩尔）表示的摩尔比为100以上;

7. 发明公开

EP1838661A1 NORBORNANE BASED CYCLOALIPHATIC COMPOUNDS CONTAINING METHYLENE AMINE GROUPS 审中-公开
标题翻译：甲基丙烯酸环己烯酯
公开(公告)号：EP1838661A1
公开(公告)日：2007-10-03
申请号：EP05711685.7
申请日：2005-01-20
申请人： E.I. du Pont de Nemours and Company
发明人： ALLGEIER, Alan, Martin , LENGES, Christian, Peter
IPC分类号： C07C211/19 , C07C215/20 , C07C209/48 , C07C229/46 , C07D307/33 , C07C255/47 , C07C255/61
CPC分类号： C07C229/46 , C07C211/19 , C07C211/26 , C07C215/20 , C07C2601/14 , C07C2602/42
摘要： The present invention relates to novel norbornane based cycloaliphatic methylene amine compounds, and methods for making the same using nitrile hydrogenation reactions.
摘要翻译：本发明涉及新型降冰片烷基脂环族亚甲基胺化合物及其制备方法。

8. 发明授权

EP0812190B1 R-ENANTIOMER OF N-PROPARGYL-1-AMINOINDAN FOR THE TREATMENT OF VARIOUS DISEASES AND MESYLATE, ESYLATE AND SULFATE THEREOF 失效
标题翻译： R-ENANTIMER DES N-PROPARGYL-1-AMINOINDAN ZUR BEHANDLUNG VERSCHIEDENER KRANKHEITEN UND MESYLAT，ESYLAT UND SULFAT DAVON
公开(公告)号：EP0812190B1
公开(公告)日：2004-12-08
申请号：EP95903505.6
申请日：1994-10-12
申请人： TEVA PHARMACEUTICAL INDUSTRIES, LTD. , TECHNION RESEARCH AND DEVELOPMENT FOUNDATION, LTD.
发明人： YOUDIM, Moussa B.H. , FINBERG, John P.M. , LEVY, Ruth , STERLING, Jeffrey , LERNER, David , BERGER-PASKIN, Tirtsah , YELLIN, Haim , VEINBERG, Alex
IPC分类号： A61K31/135 , A61K31/195 , C07C211/19 , C07C211/30
CPC分类号： C07C211/30 , A61K31/195 , A61K31/215 , A61K45/06 , C07C2602/08 , Y02A50/395 , A61K2300/00
摘要： The subject invention provides R(+)-N-propargyl-1-aminoindan and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions containing same. The subject invention also provides methods of treating a subject afflicted with Parkinson's disease, a memory disorder, dementia, depression, hyperactive syndrome, an affective illness, a neurodegenerative disease, a neurotoxic injury, brain ischemia, a head trauma injury, a spinal trauma injury, schizophrenia, an attention deficit disorder, multiple sclerosis, or withdrawal symptoms, using R(+)-N-propargyl-1-aminoindan or the pharmaceutically acceptable salt of the subject invention. The subject invention further provides a method of preventing nerve damage in a subject. Finally, the subject invention provides methods of preparing R(+)-N-propargyl-1-aminoindan, a salt thereof, and racemic N-propargyl-1-aminoindan.
摘要翻译：本发明提供R（+） - N-炔丙基-1-氨基茚满及其药学上可接受的盐，以及含有它们的药物组合物。本发明还提供了治疗患有帕金森病，记忆障碍，痴呆，抑郁症，多动症综合征，情感疾病，神经变性疾病，神经毒性损伤，脑缺血，头部创伤损伤，脊髓损伤损伤，精神分裂症，注意力缺陷障碍，多发性硬化症或戒断症状，使用本发明的R（+） - N-炔丙基-1-氨基茚满或其药学上可接受的盐。本发明还提供一种预防受试者的神经损伤的方法。最后，本发明提供了制备R（+） - N-炔丙基-1-氨基茚满及其盐和外消旋的N-炔丙基-1-氨基茚满的方法。

9. 发明授权

EP2708527B1 ALDEHYDE COMPOUND PRODUCTION METHOD 有权
公开(公告)号：EP2708527B1
公开(公告)日：2019-03-20
申请号：EP12782970.3
申请日：2012-05-07
申请人： Mitsui Chemicals, Inc.
发明人： KUMA, Shigetoshi , SAKATA, Michiharu , TOKUNAGA, Kouichi , SHIMAKAWA, Chitoshi , KAKINUMA, Naoyuki , FURUYA, Masayuki , TANAKA, Mamoru
IPC分类号： C07C45/49 , C07C47/347 , C07C209/26 , C07C209/48 , C07C211/19 , C07C253/30 , C07C255/47 , C07C263/10 , C07C265/14 , C07B61/00 , C07C45/29 , C07C209/52

10. 发明公开

EP3114107A4 PROPELLANE DERIVATES AND SYNTHESIS 有权转让
公开(公告)号：EP3114107A4
公开(公告)日：2017-11-01
申请号：EP15757721
申请日：2015-03-05
申请人： KALYRA PHARMACEUTICALS INC
发明人： BUNKER KEVIN DUANE
IPC分类号： C07C61/125 , C07C45/44 , C07C47/347 , C07C211/19 , C07C211/35 , C07C229/28 , C07C235/26 , C07C247/14 , C07C251/42 , C07C255/46 , C07C255/64 , C07C271/22 , C07D249/06
CPC分类号： C07D249/06 , C07C29/00 , C07C31/137 , C07C45/44 , C07C47/347 , C07C209/26 , C07C209/48 , C07C211/19 , C07C211/35 , C07C227/04 , C07C229/28 , C07C247/14 , C07C249/04 , C07C251/40 , C07C251/42 , C07C253/00 , C07C255/31 , C07C255/46 , C07C255/47 , C07C255/64 , C07C269/00 , C07C271/22 , C07C2602/38
摘要： Disclosed herein are compounds of the general Formula (I), and methods of synthesizing substituted bicyclo[1.1.1 jpentanes. The synthetic methods described herein use a [1.1.1]propellane, a Group VIII transition metal compound, a hydride source and a reagent that can contribute a substituent to form a substituted bicyclo[1.1.1]pentane, such as a compound of the general Formula (I).

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