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1. 发明申请

WO9932429A3 METHOD FOR PRODUCING SECONDARY AMINES FROM NITRILES AND PRIMARY AMINES 审中-公开
标题翻译：用于生产仲胺由伯胺和腈
公开(公告)号：WO9932429A3
公开(公告)日：1999-08-26
申请号：PCT/EP9808248
申请日：1998-12-16
申请人： BASF AG , FUCHS EBERHARD , BREITSCHEIDEL BORIS , OHLBACH FRANK , STEFFEN FRANK , HUNGER JUERGEN
发明人： FUCHS EBERHARD , BREITSCHEIDEL BORIS , OHLBACH FRANK , STEFFEN FRANK , HUNGER JUERGEN
IPC分类号： C07C209/48 , C07C211/08 , C07C211/34
CPC分类号： C07C209/48 , C07C2601/14 , C07C211/08 , C07C211/34
摘要： The invention relates to a method for producing amines of general formula (I) X(-CH2-NHR)n in which R independently represents C1-200-alkyl, C3-8-cycloalkyl, C4-20-alkyl cycloalkyl, C4-20-cylcoalkyl alkyl, C2-20-alkoxyalkyl, aryl, C7-20-alkylaryl, C7-20-aryl alkyl, C2-8-hyrodoxyalkyl, C2-8-mercaptoalkyl, C8-20-aryloxyalkyl or jointly represents a saturated or unsaturated C2-6-alkylene chain which is optionally substituted singly to triply by C1-4-alkyl and is optionally interrupted by oxygen or nitrogen. X is a C1-20-alkyl, C2-20-alkenyl or C3-8-cycloalkyl with n free valances optionally substituted by C1-20-alkyl, C3-8-cycloalkyl, C4-20-alkyl cycloalkyl, C4-20-cycloalkyl alkyl, C2-20-alkoxyalkyl, aryl, C7-20-alkylaryl, C7-20-aryl alkyl, C1-20-alkoxy, hydroxy, C1-20-hyrodoxyalkyl, amino, C1-20-alkyl amino, C2-20-dialkyl amino, C2-12-alkenyl amino, C3-8-cycloalkyl amino, aryl amino, diaryl amino, aryl-C1-8-alkyl amino, halogen, mercapto, C2-20-alkenyloxy, C3-8-cycloalkoxy, aryloxy, and C2-8-alkoxycarbonyl, and n is a whole number from 1 to 4. The amines are produced by reacting nitriles of general formula (II) X(-CN)n in which X and n have the above mentioned meanings with primary amines of general formula (III) H2NR in which R has the above mentioned meanings, and with hydrogen at temperatures ranging from 50 to 250 DEG C and pressure ranging from 5 to 350 bar in the presence of a catalyst containing Pd, whereby the catalyst comprises 0.1 to 10 wt. % Pd on a carrier, said wt. % being relative to the total weight of the catalyst.
摘要翻译：一种制备通式的胺（I）X（CH 2 NHR）n，其中R独立地C1-200烷基，C 3-8环烷基，C 4-20烷基环烷基，C 4-20环烷基烷基，C2过程 20烷氧基烷基，芳基，C7-20烷基芳基，C7-20芳烷基，C2-8羟基烷基，C2-8巯基烷基，C 8-20芳氧基烷基或一起任选地被单取代由C 1-4 - 烷基取代的三取代饱和或不饱和，任选地被氧或氮C 2-6亚平均X是任选被C 1-20烷基取代的，C 3-8环烷基，C 4-20烷基环烷基，C 4-20环烷基烷基，C 2-20烷氧基烷基中断芳基，C7-20烷基芳基，C7-20芳烷基，C1-20烷氧基，羟基，C 1-20羟基烷基，氨基，C 1-20烷基氨基，C 2-20二烷基氨基，C 2-12 - 烯基，C3 8环烷基氨基，芳氨基，二芳基氨基，芳基-C 1-8 - 烷基氨基，卤素，巯基，C 2-20链烯氧基，C 3-8 - 环烷氧基，芳氧基，C2-8烷氧羰基取代的C 1-20 - 烷基，C 2-20 - 链烯基或C 3-8 - 环烷基，其中n自由价并且n是从1到4的整数，通过使通式腈（II）X（-CN）n，其中X和n具有以上给出的含义，与通式的伯胺（III）H 2 NR ，其中R具有上述含义，并在温度为50至5〜350巴的含Pd催化剂的存在下250℃，氢气压力，其中，基于所述催化剂的总重量计所述催化剂为0.1〜10重量包含.-在支撑％的Pd。

2. 发明申请

WO2013163892A1 NOVEL TRIAZOLO PYRIMIDINE COMPOUNDS AND A PROCESS OF PREPARATION THEREOF 审中-公开
标题翻译：新型三唑吡啶化合物及其制备方法
公开(公告)号：WO2013163892A1
公开(公告)日：2013-11-07
申请号：PCT/CN2013/000495
申请日：2013-05-02
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： WANG, Hailong , WANG, Zhongqing , SHI, Jing , KONG, Kailai , WANG, Zhigang
IPC分类号： C07D247/02 , C07D317/44 , C07D487/04 , C07C209/58 , C07C211/34
CPC分类号： C07C209/58 , C07B2200/07 , C07C259/08 , C07C2601/02 , C07D239/47 , C07D317/44 , C07D405/12 , C07D487/04 , C07F5/025 , C07C211/40
摘要： Provided is a pyrimidine compound of formula (I) useful as a pharmaceutical intermediate, wherein Q is selected from the following groups: -C(R 1 R 2 ), -(C=0), -BR 3 . Also provided are a process for preparing said pyrimidine compound, intermediates used in said process, and the use of said pyrimidine compound in the preparation of ticagrelor.
摘要翻译：提供可用作药物中间体的式（I）嘧啶化合物，其中Q选自以下基团：-C（R 1 R 2）， - （C = O），-BR 3。还提供了制备所述嘧啶化合物的方法，所述方法中使用的中间体以及所述嘧啶化合物在制备替卡格雷中的用途。

3. 发明申请

WO00035279A1 EXO-S-MECAMYLAMINE FORMULATION AND USE IN TREATMENT 审中-公开
公开(公告)号：WO00035279A1
公开(公告)日：2000-06-22
申请号：PCT/US1999/030153
申请日：1999-12-16
IPC分类号： A61K9/06 , A01N33/02 , A01N33/18 , A01N33/24 , A61K9/08 , A61K9/22 , A61K9/52 , A61K31/015 , A61K31/13 , A61P1/04 , A61P1/06 , A61P3/02 , A61P9/12 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P35/00 , A61P37/08 , C07C209/88 , C07C211/34 , C07D217/26
CPC分类号： A61K31/13 , A61K9/0019 , A61K31/015 , C07D401/04
摘要： A pharmaceutical composition includes a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-R-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-S-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-R-mecamylamine, said amount being sufficient to ameliorate the medical condition. The medical conditions include but are not limited to substance addiction (involving nicotine, cocaine, alcohol, amphetamine, opiate, other psychostimulant and a combination thereof), aiding smoking cessation, treating weight gain associated with smoking cessation, hypertension, hypertensive crisis, Tourette's Syndrome and other tremors, cancer (such as small cell lung cancer), atherogenic profile, neuropsychiatric disorders (such as bipolar disorder, depression, an anxiety disorder, schizophrenia, a seizure disorder, Parkinson's disease and attention deficit hyperactivity disorder), chronic fatigue syndrome, Crohn's disease, autonomic dysreflexia, and spasmogenic intestinal disorders.
摘要翻译：药物组合物包含治疗有效量的外消旋S-甲基胺或其药学上可接受的盐，其与药学上可接受的载体组合基本上不含外消旋麦角胺。优选的量为约0.5mg至约20mg。医疗条件通过施用治疗有效量的基本上不含其外消旋甲基氨基甲酰胺的外-S-美加胺或其药学上可接受的盐来治疗，所述量足以改善医疗状况。医疗条件包括但不限于物质成瘾（涉及尼古丁，可卡因，酒精，苯丙胺，阿片剂，其他精神兴奋剂及其组合），帮助戒烟，治疗与戒烟相关的体重增加，高血压，高血压危象，Tourette综合征其他震颤，癌症（如小细胞肺癌），致动脉粥样化特征，神经精神障碍（如双相情感障碍，抑郁症，焦虑症，精神分裂症，癫痫发作障碍，帕金森病和注意缺陷多动障碍），慢性疲劳综合征，克罗恩病，自主神经反射异常和痉挛性肠道疾病。

4. 发明申请

WO1996008462A1 METHOD OF INCREASING HYDROGENATION RATE OF AROMATIC AMINES 审中-公开
标题翻译：增加芳族氨基酸加氢速率的方法
公开(公告)号：WO1996008462A1
公开(公告)日：1996-03-21
申请号：PCT/US1995010851
申请日：1995-08-28
申请人： OLIN CORPORATION
发明人： OLIN CORPORATION , WHITMAN, Peter, J.
IPC分类号： C07C211/34
CPC分类号： C07C211/36 , C07C209/72
摘要： A process for increasing the rate of catalytic hydrogenation of aromatic amines by reacting aromatic amines with hydrogen in the presence of a noble metal catalyst, a water miscible organic solvent, lithium hydroxide catalyst promoter, and water in an effective amount to increase the rate of the hydrogenation reaction without an appreciable increase in total amounts of by-products.
摘要翻译：在贵金属催化剂，水混溶性有机溶剂，氢氧化锂催化剂促进剂和水的存在下，通过使芳族胺与氢反应，在有效量下增加芳香族胺的催化氢化速率的方法，氢化反应而副产物总量不会明显增加。

5. 发明申请

WO00035280A1 EXO-R-MECAMYLAMINE FORMULATION AND USE IN TREATMENT 审中-公开
公开(公告)号：WO00035280A1
公开(公告)日：2000-06-22
申请号：PCT/US1999/030137
申请日：1999-12-16
IPC分类号： A61K9/06 , A01N33/02 , A01N33/18 , A01N33/24 , A61K9/08 , A61K9/22 , A61K9/52 , A61K31/015 , A61K31/13 , A61P1/04 , A61P1/06 , A61P3/02 , A61P9/12 , A61P25/02 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P35/00 , A61P37/08 , C07C209/88 , C07C211/34 , C07D217/26
CPC分类号： A61K31/13 , A61K9/0019 , A61K31/015 , C07D401/04
摘要： A pharmaceutical composition includes a therapeutically effective amount of exo-R-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of exo-S-mecamylamine in combination with a pharmaceutically acceptable carrier. Preferably the amount is about 0.5 mg to about 20 mg. Medical conditions are treated by administering a therapeutically effective amount of exo-R-mecamylamine or a pharmaceutically acceptable salt thereof, substantially free of its exo-S-mecamylamine, said amount being sufficient to ameliorate the medical condition. The medical conditions include but are not limited to substance addiction (involving nicotine, cocaine, alcohol, amphetamine, opiate, other psychostimulant and a combination thereof), aiding smoking cessation, treating weight gain associated with smoking cessation, hypertension, hypertensive crisis, Tourette's Syndrome and other tremors, cancer (such as small cell lung cancer), atherogenic profile, neuropsychiatric disorders (such as bipolar disorder, depression, an anxiety disorder, schizophrenia, a seizure disorders, Parkinson's disease and attention deficit hyperactivity disorder), chronic fatigue syndrome, Crohn's disease, autonomic dysreflexia, and spasmogenic intestinal disorders.
摘要翻译：药物组合物包含治疗有效量的外消旋-N-甲基胺或其药学上可接受的盐，其基本上不含外-S-麦考胺与药学上可接受的载体。优选地，该量为约0.5mg至约20mg。通过施用治疗有效量的基本上不含其外-S-麦卡胺的外消旋美沙酮胺或其药学上可接受的盐来治疗医学病症，所述量足以改善医疗状况。医疗条件包括但不限于物质成瘾（涉及尼古丁，可卡因，酒精，苯丙胺，阿片剂，其他精神兴奋剂及其组合），帮助戒烟，治疗与戒烟相关的体重增加，高血压，高血压危象，Tourette综合征其他震颤，癌症（如小细胞肺癌），致动脉粥样硬化症状，神经精神障碍（如双相情感障碍，抑郁症，焦虑症，精神分裂症，癫痫发作障碍，帕金森病和注意缺陷多动障碍），慢性疲劳综合征，克罗恩病，自主神经反射异常和痉挛性肠道疾病。

6. 发明申请

WO99032429A2 METHOD FOR PRODUCING SECONDARY AMINES FROM NITRILES AND PRIMARY AMINES 审中-公开
标题翻译：从硝酸和原胺生产仲胺的方法
公开(公告)号：WO99032429A2
公开(公告)日：1999-07-01
申请号：PCT/EP1998/008248
申请日：1998-12-16
IPC分类号： C07C209/48 , C07C211/08 , C07C211/34
CPC分类号： C07C209/48 , C07C2601/14 , C07C211/08 , C07C211/34
摘要： The invention relates to a method for producing amines of general formula (I) X(-CH2-NHR)n in which R independently represents C1-200-alkyl, C3-8-cycloalkyl, C4-20-alkyl cycloalkyl, C4-20-cylcoalkyl alkyl, C2-20-alkoxyalkyl, aryl, C7-20-alkylaryl, C7-20-aryl alkyl, C2-8-hyrodoxyalkyl, C2-8-mercaptoalkyl, C8-20-aryloxyalkyl or jointly represents a saturated or unsaturated C2-6-alkylene chain which is optionally substituted singly to triply by C1-4-alkyl and is optionally interrupted by oxygen or nitrogen. X is a C1-20-alkyl, C2-20-alkenyl or C3-8-cycloalkyl with n free valances optionally substituted by C1-20-alkyl, C3-8-cycloalkyl, C4-20-alkyl cycloalkyl, C4-20-cycloalkyl alkyl, C2-20-alkoxyalkyl, aryl, C7-20-alkylaryl, C7-20-aryl alkyl, C1-20-alkoxy, hydroxy, C1-20-hyrodoxyalkyl, amino, C1-20-alkyl amino, C2-20-dialkyl amino, C2-12-alkenyl amino, C3-8-cycloalkyl amino, aryl amino, diaryl amino, aryl-C1-8-alkyl amino, halogen, mercapto, C2-20-alkenyloxy, C3-8-cycloalkoxy, aryloxy, and C2-8-alkoxycarbonyl, and n is a whole number from 1 to 4. The amines are produced by reacting nitriles of general formula (II) X(-CN)n in which X and n have the above mentioned meanings with primary amines of general formula (III) H2NR in which R has the above mentioned meanings, and with hydrogen at temperatures ranging from 50 to 250 DEG C and pressure ranging from 5 to 350 bar in the presence of a catalyst containing Pd, whereby the catalyst comprises 0.1 to 10 wt. % Pd on a carrier, said wt. % being relative to the total weight of the catalyst.
摘要翻译：一种制备通式的胺（I）X（CH 2 NHR）n，其中R独立地C1-200烷基，C 3-8环烷基，C 4-20烷基环烷基，C 4-20环烷基烷基，C2过程 20烷氧基烷基，芳基，C7-20烷基芳基，C7-20芳烷基，C2-8羟基烷基，C2-8巯基烷基，C 8-20芳氧基烷基或一起任选地被单取代由C 1-4 - 烷基取代的三取代饱和或不饱和，任选地被氧或氮C 2-6亚平均X是任选被C 1-20烷基取代的，C 3-8环烷基，C 4-20烷基环烷基，C 4-20环烷基烷基，C 2-20烷氧基烷基中断芳基，C7-20烷基芳基，C7-20芳烷基，C1-20烷氧基，羟基，C 1-20羟基烷基，氨基，C 1-20烷基氨基，C 2-20二烷基氨基，C 2-12 - 烯基，C3 8环烷基氨基，芳氨基，二芳基氨基，芳基-C 1-8 - 烷基氨基，卤素，巯基，C 2-20链烯氧基，C 3-8 - 环烷氧基，芳氧基，C2-8烷氧羰基取代的C 1-20 - 烷基，C 2-20 - 具有n个游离价的烯基或C3-8环烷基并且n是从1到4的整数，通过使通式腈（II）X（-CN）n，其中X和n具有以上给出的含义，与通式的伯胺（III）H 2 NR ，其中R具有上述含义，并在温度为50至5〜350巴的含Pd催化剂的存在下250℃，氢气压力，其中，基于所述催化剂的总重量计所述催化剂为0.1〜10重量 .-％载体上的Pd。

7. 发明申请

WO1998017625A1 NOVEL REMEDIES FOR INFECTIOUS DISEASES 审中-公开
标题翻译：感染性疾病的新措施
公开(公告)号：WO1998017625A1
公开(公告)日：1998-04-30
申请号：PCT/JP1997003812
申请日：1997-10-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , OHTA, Toshiharu , NAKAYAMA, Kiyoshi , OHTSUKA, Masami , INAGAKI, Hiroaki , NISHI, Toshiyuki , ISHIDA, Yohhei
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C211/34
CPC分类号： C07D207/14 , C07C237/42
摘要： Novel compounds having three substituents in the cyclic partial structure thereof, such as a pyrrolidine or a benzene ring, for example, homophenylalanyl-trans-4-((S)-3-amino-2-hydroxypropionylamino)proline 5-indanylamide and N-(3-phenylpropyl)-3-((S)-2-hydroxy-3-aminopropionylamino)-5-(D-homophenylalanylamino)-benzamide. These compounds act on pathogenic microorganisms which have acquired tolerance to the existing antimicrobials and elevate the sensitivity to the antimicrobials, thus making them nontolerant. When used together with the antimicrobials, these compounds can efficaciously establish the prevention and/or treatment of microbial infectious diseases.
摘要翻译：具有其环状部分结构中的三个取代基的新型化合物，例如吡咯烷或苯环，例如高苯丙氨酰 - 反式-4 - （（S）-3-氨基-2-羟基丙酰基氨基）脯氨酸5-茚满酰胺和N- （3-苯基丙基）-3 - （（S）-2-羟基-3-氨基丙酰氨基）-5-（D-homophenylalanylamino） - 苯甲酰胺。这些化合物对已经获得对现有抗微生物剂的耐受性并提高对抗微生物剂的敏感性的致病微生物起作用，使其不耐受。当与抗微生物剂一起使用时，这些化合物可以有效地建立预防和/或治疗微生物感染性疾病。

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