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1. 发明申请

WO0238105A3 NOVEL POLYAMINE ANALOG-AMINO ACID CONJUGATES USEFUL AS ANTICANCER AGENTS 审中-公开
标题翻译：新型聚氨酯类似物 - 氨基酸连接作为防治剂
公开(公告)号：WO0238105A3
公开(公告)日：2003-02-27
申请号：PCT/US0143585
申请日：2001-11-08
申请人： SLIL BIOMEDICAL CORP , FRYDMAN BENJAMIN , MARTON LAURENCE J , VALASINAS ALDONIA L , REDDY VENODHAR K
发明人： FRYDMAN BENJAMIN , MARTON LAURENCE J , VALASINAS ALDONIA L , REDDY VENODHAR K
IPC分类号： A61K38/00 , A61K31/16 , A61K47/48 , A61P35/00 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C237/10 , C07C257/18 , C07D233/54 , C07C211/13 , A61K31/13 , A61K31/14 , A61K31/495 , A61K31/50 , A61K31/70
CPC分类号： C07C237/10 , A61K47/542 , A61K47/64
摘要： Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.
摘要翻译：提供多胺类似物与氨基酸缀合的缀合物，以及包含这些缀合物的组合物。还提供了使用这些缀合物作为抗癌治疗的方法。

2. 发明申请

WO2013006143A1 PROCESS FOR PRODUCING AN AMINOPROPYNE OR ENAMINONE 审中-公开
标题翻译：生产氨基丙烯或诺曼酮的方法
公开(公告)号：WO2013006143A1
公开(公告)日：2013-01-10
申请号：PCT/SG2012/000240
申请日：2012-07-06
申请人： AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH , ZHANG, Yugen , YU, Dingyi , LIN, Zhewang
发明人： ZHANG, Yugen , YU, Dingyi , LIN, Zhewang
IPC分类号： C07C209/66 , C07C211/23 , C07C255/50 , C07D295/03 , C07D207/06 , C07D211/14 , C07D249/06 , C07B37/00
CPC分类号： C07C209/66 , C07B37/02 , C07C209/78 , C07C213/08 , C07C253/30 , C07D207/04 , C07D249/04 , C07D249/06 , C07D295/023 , C07D295/03 , C07C211/27 , C07C211/29 , C07C211/35 , C07C255/58 , C07C217/58
摘要： There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50°C to 150°C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.
摘要翻译：提供了一种制备氨基丙炔或烯胺的方法，包括在过渡金属催化剂存在下使金属乙炔，胺和含羰基化合物反应的步骤。还提供了一种制备氨基丙炔的方法，包括在过渡金属催化剂存在下，在50℃至150℃的反应温度下，使金属乙炔，胺和含卤素化合物反应的步骤。还提供了进一步合成产生的氨基丙炔以获得丁炔胺，另一种氨基丙炔或三唑的方法。

3. 发明申请

WO9903817B1 ALIPHATIC PROPARGYLAMINES AS CELLULAR RESCUE AGENTS 审中-公开
标题翻译：作为细胞拯救剂的脂肪族丙烷胺
公开(公告)号：WO9903817B1
公开(公告)日：1999-07-01
申请号：PCT/CA9800683
申请日：1998-07-14
申请人： UNIV SASKATCHEWAN , PATERSON I ALICK , DURDEN DAVID A , DAVIS BRUCE A , DYCK LILLIAN E , YU PETER H , LI XIN MIN , BOULTON ALAN A
发明人： PATERSON I ALICK , DURDEN DAVID A , DAVIS BRUCE A , DYCK LILLIAN E , YU PETER H , LI XIN-MIN , BOULTON ALAN A
IPC分类号： A61P9/00 , A61K31/13 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P43/00 , C07C211/23
CPC分类号： C07C211/23
摘要： The present invention relates to the use of a group of propargylamines of general formula (I) wherein R is hydrogen or CH3 and R is (CH2)nCH3 and n is an integer from 0 to 16, and salts thereof, as cellular rescue agents in the treatment and prevention of diseases in which cell death occurs by apoptosis. Some of the compounds of formula (I) are novel. The invention is also directed to the use of these compounds in the treatment of these diseases, as well as to processes for the preparation of the compounds.
摘要翻译：本发明涉及一组通式（I）的炔丙胺的用途，其中R 1是氢或CH 3且R 2是（CH 2）n CH 3且n是0-16的整数，及其盐作为细胞拯救剂用于治疗和预防细胞死亡通过凋亡发生的疾病。式（I）的一些化合物是新颖的。本发明还涉及这些化合物在治疗这些疾病中的用途，以及制备这些化合物的方法。

4. 发明申请

WO2012005692A1 PROPARGYLAMINE SYNTHESIS USING A COPPER (I) CATALYSED THREE COMPONENT COUPLING REACTION 审中-公开
标题翻译：使用铜（I）催化的三元组件联合反应的丙烯酰胺合成
公开(公告)号：WO2012005692A1
公开(公告)日：2012-01-12
申请号：PCT/SG2011/000237
申请日：2011-07-06
申请人： AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH , ZHANG, Yugen , YU, Dingyi
发明人： ZHANG, Yugen , YU, Dingyi
IPC分类号： C07C209/66 , C07C211/25 , C07C211/35 , C07C211/23 , C07C211/26
CPC分类号： C07C209/66 , C07C2601/14 , C07C211/23 , C07C211/25 , C07C211/28
摘要： The present invention relates to a three component coupling reaction. In this reaction a terminal alkyne or a salt thereof, a geminal dihalide and a primary or secondary amine are reacted in the presence of a copper (I) catalyst to produce a propargylamine.
摘要翻译：本发明涉及三组分偶联反应。在该反应中，末端炔或其盐，偕二卤化物和伯胺或仲胺在铜（I）催化剂的存在下反应生成炔丙胺。

5. 发明申请

WO0066587A3 POLYAMINES AND THEIR USE IN THERAPY 审中-公开
标题翻译：聚氨酯及其在治疗中的应用
公开(公告)号：WO0066587A3
公开(公告)日：2001-01-25
申请号：PCT/US0011591
申请日：2000-04-27
申请人： SLIL BIOMEDICAL CORP , FRYDMAN BENJAMIN , MARTON LAURENCE J , REDDY VENODHAR K , VALASINAS ALDONIA , BLOKHIN ANDREI V , BASU HIRAK S
发明人： FRYDMAN BENJAMIN , MARTON LAURENCE J , REDDY VENODHAR K , VALASINAS ALDONIA , BLOKHIN ANDREI V , BASU HIRAK S
IPC分类号： A61K31/13 , A61K31/132 , A61K31/137 , A61K31/155 , A61K31/40 , A61K31/409 , A61K38/00 , A61K47/48 , A61P1/04 , A61P9/10 , A61P17/02 , A61P17/06 , A61P25/08 , A61P25/28 , A61P31/04 , A61P33/00 , A61P35/00 , C07C45/46 , C07C67/343 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C251/18 , C07C257/18 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07K5/103 , C07K7/06
CPC分类号： C07C211/09 , A61K38/00 , A61K47/65 , C07C45/46 , C07C67/343 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C257/18 , C07C2601/04 , C07C2601/08 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要翻译：提供新的构象限制性多胺类似物，以及包含这些新型多胺类似物的组合物。还提供了将新型多胺类似物用于治疗诸如癌症的疾病的方法。还提供了通过将多胺类似物与卟啉化合物共价连接并与新型多胺 - 卟啉共价缀合物一起将这些类似物特异性递送至肿瘤细胞的方法。

6. 发明申请

WO03018525B1 PHOTORESPONSIVE POLYMER, BUILT-UP TYPE DIACETYLENE POLYMER, CRYSTALS OF AMMONIUM CARBOXYLATES, AND PROCESSES FOR PRODUCTION OF THEM 审中-公开
标题翻译：聚对苯二甲酸乙二醇酯聚合物，内置型二乙烯聚合物，羧甲基纤维素的结晶及其生产工艺
公开(公告)号：WO03018525B1
公开(公告)日：2003-09-18
申请号：PCT/JP0208559
申请日：2002-08-26
申请人： JAPAN SCIENCE & TECH CORP , MATSUMOTO AKIKAZU , ODANI TORU
发明人： MATSUMOTO AKIKAZU , ODANI TORU
IPC分类号： C08F2/48 , C08G61/08 , C08G73/00 , C07C51/41 , C07C57/10 , C07C57/16 , C07C57/24 , C07C211/03 , C07C211/23 , C07C211/27 , C07C211/35 , C08F36/04 , C08F38/02 , C08J3/20
CPC分类号： C08G61/08 , C08G73/00
摘要： Crystals of ammonium carboxylates are produced by mixing crystals of a carboxyl-bearing conjugated diene such as muconic acid with at least one compound selected from among amines and ammonia in the absence of a liquid medium. The use of an amine having a bivalent group represented by the general formula: -Ar-N=N-Ar'- wherein Ar and Ar' are each independently a bivalent aromatic hydrocarbon group as the above amine component gives a novel photoresponsive polymer which comprises layer crystals of a carboxyl-bearing conjugated diene polymer and the amine intercalated thereinto. Further, a built-up type diacetylene polymer is obtained by subjecting crystals of an ammonium carboxylate prepared from a carboxylic acid and an amine, at least either of which is a diacetylene derivative, to irradiation with light or heating.
摘要翻译：羧酸铵的晶体通过在不存在液体介质的情况下将含羧基的共轭二烯如粘康酸的晶体与选自胺和氨中的至少一种化合物混合来制备。使用由以下通式表示的二价基团的胺：-Ar-N = N-Ar'-其中Ar和Ar'各自独立地为作为上述胺组分的二价芳族烃基，得到新的光响应聚合物，其包含含羧基共轭二烯聚合物的层状晶体和插入其中的胺。此外，通过使由羧酸和胺制备的羧酸铵的结晶（其中至少一种是二乙炔衍生物）进行光照射或加热，得到积层型乙炔聚合物。

7. 发明申请

WO99028034A1 METHOD FOR PREPARING A CATALYST AND CATALYSTS PREPARED ACCORDINGLY 审中-公开
标题翻译：一种用于生产催化剂和这种方法获得的催化剂
公开(公告)号：WO99028034A1
公开(公告)日：1999-06-10
申请号：PCT/EP1998/007785
申请日：1998-12-01
IPC分类号： B01J23/84 , B01J31/22 , C07B61/00 , C07C29/42 , C07C33/042 , C07C209/60 , C07C211/23 , C07C213/00 , C07C213/02 , C07C215/24
CPC分类号： B01J31/1616 , B01J31/2286 , B01J2231/346 , B01J2531/10 , B01J2531/16 , B01J2531/20 , C07C29/42 , C07C209/60 , C07C213/00 , C07C211/23 , C07C215/24 , C07C33/042 , C07C33/046
摘要： The invention relates to a method for preparing a catalyst through activation of a catalytic material comprising a) at least one metal from the first or second side group or one compound thereof and b) optionally a carrier. This catalyst is characterised in that the material is treated with an alkine of formula (I): R1-CC-R , in which R represents alkyl, cycloalkyl, aryl, hydroxyalkyl, alkyl halide, alkoxy or alkoxyalkyl, R represents hydrogen, alkyl, cycloalkyl or aryl, as well as with a carbonyl compound of formula (II), in which R and R represent independently from each other hydrogen, alkyl, alkyl halide, cycloalkyl or aryl. The invention also relates to catalysts obtained according to said method, and to alkinylations and aminoalkylations using said catalysts.
摘要翻译：本发明涉及一种用于通过激活的催化组合物，其包括制备催化剂的方法）任选地包括在所述第一或第二子基或其化合物中的至少一种金属，b）载体，其特征在于，所述质量块是（I）式的炔烃，R <1> -CC-R <2>其中，R <1>是烷基，环烷基，芳基，羟烷基，卤代烷基，烷氧基或烷氧基烷基，R <2>代表氢原子，烷基，环烷基或芳基，和式（II）的羰基化合物，其中R <3>和R <4>独立地是氢原子，烷基，卤代烷基，环烷基或芳基，通过该方法的催化剂和炔基，并使用这些aminoalkylations处理获得催化剂。

8. 发明申请

WO1992015551A1 ALIPHATIC PROPARGYLAMINES AS SELECTIVE MAO-B INHIBITORS AND AS NEUROPROTECTIVE AGENTS 审中-公开
标题翻译：作为选择性MAO-B抑制剂和神经保护剂的ALIPHATIC PROPARGYLAMINES
公开(公告)号：WO1992015551A1
公开(公告)日：1992-09-17
申请号：PCT/CA1992000090
申请日：1992-02-28
申请人： UNIVERSITY OF SASKATCHEWAN , YU, Peter, H. , DAVIS, Bruce, A. , BOULTON, Alan, A.
发明人： UNIVERSITY OF SASKATCHEWAN
IPC分类号： C07C211/23
CPC分类号： C07C211/23 , C07C215/08 , C07C229/12
摘要： The invention relates to a series of propargylamines, their salts and pharmaceutical compositions containing a compound of formula (III) wherein R1, R3 and R4 are the same or different and represent hydrogen or a straight chain or branched lower alkyl; y is an integer ranging from 0 to 5; z is an integer ranging from 0 to 5; and R2 is a straight chain or branched alkyl, alkenyl, alkynyl, alkoxy, alkylthio or alkyl sulphinyl group having from 3 to 11 carbon atoms, said group being unsubstituted or substituted with at least one of the substituents selected from hydroxy, aldehyde, oxo, loweracyloxy, halogen, thio, sulfoxide, sulfone, phenyl, halogen-substituted phenyl, hydroxy-substituted phenyl, cycloalkyl having from 3 to 6 carbon atoms and heterocyclic substituents having between 3 and 6 atoms, of which form 1 to 3 are heteroatoms selected from O, S and/or N, and pharmaceutically acceptable salts thereof, in admixture with a pharmaceutically acceptable carrier, excipient or adjuvant. The compounds are useful as selective monoamine oxidase B inhibitors and have demonstrated neuroprotective properties in human and veterinary medicine.
摘要翻译：本发明涉及一系列含有式（III）化合物的炔丙胺，其盐和药物组合物，其中R 1，R 3和R 4相同或不同，表示氢或直链或支链的低级烷基; y为0〜5的整数; z为0〜5的整数; 并且R 2是具有3至11个碳原子的直链或支链烷基，烯基，炔基，烷氧基，烷硫基或烷基亚磺酰基，所述基团是未取代的或被至少一个选自羟基，醛，氧代，低级酰氧基，卤素，硫代，亚砜，砜，苯基，卤素取代的苯基，羟基取代的苯基，具有3至6个碳原子的环烷基和3至6个原子的杂环取代基，其形成1至3个是选自 O，S和/或N及其药学上可接受的盐与药学上可接受的载体，赋形剂或佐剂混合。该化合物可用作选择性单胺氧化酶B抑制剂，并且已经在人和兽医学中证明了神经保护性质。

9. 发明申请

WO02038105A2 NOVEL POLYAMINE ANALOG-AMINO ACID CONJUGATES USEFUL AS ANTICANCER AGENTS 审中-公开
标题翻译：新型聚氨酯类似物 - 氨基酸连接作为防治剂
公开(公告)号：WO02038105A2
公开(公告)日：2002-05-16
申请号：PCT/US2001/043585
申请日：2001-11-08
IPC分类号： A61K38/00 , A61K31/16 , A61K47/48 , A61P35/00 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C237/10 , C07C257/18 , C07D233/54 , A61K
CPC分类号： C07C237/10 , A61K47/542 , A61K47/64
摘要： Conjugates in which polyamine analogs are conjugated to an amino acid are provided, as well as compositions comprising these conjugates. Methods of using these conjugates as anticancer treatments are also provided.
摘要翻译：提供多胺类似物与氨基酸缀合的缀合物，以及包含这些缀合物的组合物。还提供了使用这些缀合物作为抗癌治疗的方法。

10. 发明申请

WO00066587A2 CONFORMATIONALLY RESTRICTED POLYAMINE ANALOGS AS DISEASE THERAPIES 审中-公开
标题翻译：一致的限制性聚氨酯类似物作为疾病治疗
公开(公告)号：WO00066587A2
公开(公告)日：2000-11-09
申请号：PCT/US2000/011591
申请日：2000-04-27
IPC分类号： A61K31/13 , A61K31/132 , A61K31/137 , A61K31/155 , A61K31/40 , A61K31/409 , A61K38/00 , A61K47/48 , A61P1/04 , A61P9/10 , A61P17/02 , A61P17/06 , A61P25/08 , A61P25/28 , A61P31/04 , A61P33/00 , A61P35/00 , C07C45/46 , C07C67/343 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C251/18 , C07C257/18 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07K5/103 , C07K7/06
CPC分类号： C07C211/09 , A61K38/00 , A61K47/65 , C07C45/46 , C07C67/343 , C07C211/18 , C07C211/22 , C07C211/23 , C07C211/36 , C07C215/14 , C07C257/18 , C07C2601/04 , C07C2601/08 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
摘要翻译：提供新颖的构象限制性多胺类似物，以及包含这些新型多胺类似物的组合物。还提供了将新型多胺类似物用于治疗诸如癌症的疾病的方法。还提供了通过将多胺类似物共价连接到卟啉化合物以及新型多胺 - 卟啉共价缀合物将这些类似物特异性递送至肿瘤细胞的方法。

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