公开(公告)号：WO2005040177A1

公开(公告)日：2005-05-06

申请号：PCT/EP2004/052615

申请日：2004-10-21

申请人： AKZO NOBEL N.V. ,  DE KLEINE, Lambertus, A. ,  SEIFERT, Juergen, Klaus

发明人： DE KLEINE, Lambertus, A. ,  SEIFERT, Juergen, Klaus

IPC分类号： C07F9/09

CPC分类号： C07F9/12

摘要： The present invention relates to a process wherein dichloromonophenyl phosphate and monochlorodiphenyl phosphate is reacted with an aliphatic alcohol, in the presence of a Lewis acid catalyst, in the absence of solvent, at a temperature of above 60 to 200° C, and at a pressure of 0.001 to 1.1 bara, provided that the reaction mixture is sparged with an inert carrier gas if the pressure is above 0.67 bars. The present invention further relates to mixtures of monoalkyl Biphenyl phosphates and dialkyl monophenyl phosphates obtainable from this process and the use of such mixtures as a plasticiser and/or a flame retardant.

摘要翻译： 本发明涉及一种方法，其中在路易斯酸催化剂的存在下，在不存在溶剂的情况下，在高于60至200℃的温度和压力下，磷酸二苯基酯和磷酸一氯二苯酯与脂肪醇反应 为0.001至1.1巴，条件是如果压力高于0.67巴，反应混合物用惰性载气鼓泡。 本发明还涉及可从该方法获得的单烷基联苯基磷酸酯和二烷基单苯基磷酸酯的混合物，以及使用这种混合物作为增塑剂和/或阻燃剂。

公开(公告)号：WO2005012417A1

公开(公告)日：2005-02-10

申请号：PCT/KR2004/000969

申请日：2004-04-27

申请人： CHEIL INDUSTRIES INC. ,  JIN, Soon Young ,  HONG, Sang Hyun ,  AHN, Sung Hee ,  RYU, Young Sik

发明人： JIN, Soon Young ,  HONG, Sang Hyun ,  AHN, Sung Hee ,  RYU, Young Sik

IPC分类号： C08K5/5317

CPC分类号： C07F9/12 ,  C07F9/657172 ,  C08F279/02 ,  C08F279/04 ,  C08K5/51 ,  C08K5/523 ,  C08K5/527 ,  C08K5/5313 ,  C08K5/5357 ,  C08L25/04 ,  C08L51/04 ,  C08L55/02 ,  C08L2666/24 ,  C08L2666/02 ,  C08L2666/04

摘要： The flameproof resin composition according to the present invention comprises (A) 100 parts by weight of a rubber modified polystyrene resin containing (a 1 ) 20 to 100 % by weight of graft copolymer prepared by graft-polymerizing 5 to 65 parts by weight of a rubber polymer, 35 to 95 parts by weight of an aromatic vinyl monomer, 1 to 20 parts by weight of a monomer copolymerizable with said aromatic vinyl monomer and 0 to 15 parts by weight of a monomer for providing processability and heat resistance; and (a 2 ) 0 to 80 % by weight of copolymer prepared by polymerizing 60 to 90 parts by weight of an aromatic vinyl monomer, 10 to 40 parts by weight of a monomer copolymerizable with said aromatic vinyl monomer and 0 to 30 parts by weight of a monomer for providing processability and heat resistance; (B) 0.1 to 15 parts by weight of an oxaphosphorane compound; and (C) 0 to 20 parts by weight of an aromatic phosphoric acid ester compound.

摘要翻译： 根据本发明的防火树脂组合物包含（A）100重量份的橡胶改性聚苯乙烯树脂，其含有（a1）20〜100重量％的接枝共聚物，其通过将5〜65重量份的橡胶 聚合物，35〜95重量份芳族乙烯基单体，1〜20重量份可与所述芳族乙烯基单体共聚的单体和0〜15重量份用于提供加工性和耐热性的单体; 和（a2）0-80重量％的通过聚合60至90重量份芳族乙烯基单体制备的共聚物，10至40重量份可与所述芳族乙烯基单体共聚的单体和0至30重量份的 用于提供加工性和耐热性的单体; （B）0.1〜15重量份的氧化磷杂环辛烷化合物; 和（C）0〜20重量份的芳香族磷酸酯化合物。

公开(公告)号：WO2005004897A1

公开(公告)日：2005-01-20

申请号：PCT/US2004/015547

申请日：2004-05-18

申请人： VION PHARMACEUTICALS, INC. ,  LIN, Xu ,  DOYLE, Terrence, W. ,  KING, Ivan

发明人： LIN, Xu ,  DOYLE, Terrence, W. ,  KING, Ivan

IPC分类号： A61K38/16

CPC分类号： C07C311/55 ,  A61K38/04 ,  A61K38/16 ,  C07F9/12

摘要： The present invention relates to compounds according to the structure (I): Where R is -CH 3 or -CH 2 CH 2 CI; R' is C 1 -C 7 alkyl or -CH 2 CH 2 C1; R 2 or R 4 is OPO 3 H 2 , NO 2 , OCO(Glu-OH), NHCO(Glu-OH), NHR 7 and unassigned groups of R 2 , R 3 , R 4 , R 5 and R 6 are, independently, H, F, Cl, Br, I, OH, OPO 3 H 2 , OCH 3 , CF 3 , OCF 3 , NO 2 , CN, SO 2 CH 3 , SO 2 CF 3 , COCH 3 , COOCH 3 , SCH3, SF 5 , NH 2 , NHR 7 , N(CH 3 ) 2 , OP0 3 H 2 , or a C 1 -C 7 alkyl group with the proviso that when any two of unassigned groups of R 2 , R 3 , R 4 , R 5 or R 6 are other than H, the other two of unassigned groups of R 2 , R 3 , R 4 , R 5 or R 6 are H. R 7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及根据结构（I）的化合物：其中R是-CH 3或-CH 2 CH 2 Cl; R'是C 1 -C 7烷基或-CH 2 CH 2 Cl; R2或R4是OPO3H2，NO2，OCO（Glu-OH），NHCO（Glu-OH），NHR7，R2，R3，R4，R5和R6的未分配基团独立地是H，F，Cl，Br， OH，OPO3H2，OCH3，CF3，OCF3，NO2，CN，SO2CH3，SO2CF3，COCH3，COOCH3，SCH3，SF5，NH2，NHR7，N（CH3）2，OP03H2或C1-C7烷基，条件是当 R2，R3，R4，R5或R6的任何两个未分配的基团不是H，R2，R3，R4，R5或R6的另外两个未分配的基团是H.R 7是H或所述的聚谷氨酰基。 磷酸和谷氨酸可以是游离酸或其药学上可接受的盐。

公开(公告)号：WO2004078126A2

公开(公告)日：2004-09-16

申请号：PCT/US2004/006175

申请日：2004-03-01

申请人： OXIGENE, INC. ,  CHAPLIN, David, J. ,  EDVARDSEN, Klaus ,  PINNEY, Kevin, G. ,  PREZIOSO, Joseph, Anthony ,  WOOD, Mark

发明人： CHAPLIN, David, J. ,  EDVARDSEN, Klaus ,  PINNEY, Kevin, G. ,  PREZIOSO, Joseph, Anthony ,  WOOD, Mark

IPC分类号： A61K

CPC分类号： A61K31/6615 ,  A61K31/09 ,  C07C43/23 ,  C07C205/35 ,  C07D205/08 ,  C07F9/12

摘要： Novel quinone and catechol compositions, compositions containing prodrugs of quinone and catechol compositions, and methods of use for the treatment of solid tumor cancers and other vascular proliferative disorders. The disclosure particularly relates to the discovery of dual activity agents capable of generating both a vascular targeting effect and direct tumor cell cytotoxicity in order to achieve an enhanced anti-tumor response in a patient.

摘要翻译： 新型醌和儿茶酚组合物，含有醌和儿茶酚组合物的前药的组合物，以及用于治疗实体瘤癌症和其它血管增生性疾病的方法。 本公开特别涉及能够产生血管靶向效应和直接肿瘤细胞毒性的双重活性试剂的发现，以便在患者体内实现增强的抗肿瘤反应。

公开(公告)号：WO2004069146A2

公开(公告)日：2004-08-19

申请号：PCT/IL2004/000103

申请日：2004-02-03

申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM ,  ATLAS, Daphne

发明人： ATLAS, Daphne

IPC分类号： A61K

CPC分类号： A61K45/06 ,  C07C237/20 ,  C07C237/22 ,  C07F9/12

摘要： L-DOPA amide derivatives, pharmaceutical compositions containing same and their use in the treatment of conditions associated with impaired dopaminergic activity/signaling (e.g., Parkinson disease) are disclosed.

摘要翻译： 公开了L-DOPA酰胺衍生物，含有它们的药物组合物及其在治疗与多巴胺能活性/信号传导障碍（例如帕金森病）相关的病症中的用途。

公开(公告)号：WO2003063758A2

公开(公告)日：2003-08-07

申请号：PCT/IL2003/000077

申请日：2003-01-30

申请人： PHARMOS CORPORATION ,  GARZON, Aaron ,  FINK, George ,  DAR, Dalit, Esther ,  MENASHE, Naim ,  NUDELMAN, Ayelet ,  GREENBERG, Orit

发明人： GARZON, Aaron ,  FINK, George ,  DAR, Dalit, Esther ,  MENASHE, Naim ,  NUDELMAN, Ayelet ,  GREENBERG, Orit

IPC分类号： A61K

CPC分类号： C07C255/40 ,  A61K31/12 ,  A61K31/35 ,  C07C39/23 ,  C07C45/292 ,  C07C45/54 ,  C07C45/71 ,  C07C49/657 ,  C07C49/747 ,  C07C49/753 ,  C07C69/30 ,  C07C69/40 ,  C07C69/60 ,  C07C251/44 ,  C07C2602/42 ,  C07F9/12

摘要： The present invention relates to non-classical cannabinoids that are ligands of the peripheral cannabinoid receptor CB2, and to pharmaceutical compositions thereof comprising as an active ingredient novel (+) α-pinene derivatives, which are useful for prevention and treatment of autoimmune diseases including but not limited to rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, myasthenia gravis, diabetes mellitus type I, hepatitis, psoriasis, tissue rejection in organ transplants, malabsorption syndromes such as celiac disease, pulmonary diseases such as asthma and Sjögren's syndrome, inflammation including inflammatory bowel disease, pain including peripheral, visceral, neurophathic inflammatory and referred pain, muscle spasticity, cardiovascular disorders including arrhythmia, hypertension and myocardial ischemia, neurological disorders including stroke, migraine and cluster headaches, neurodegenerative diseases including Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's chorea, prion-associated neurodegeneration, CNS poisoning and certain types of cancer.

摘要翻译： 本发明涉及作为外周大麻素受体CB2的配体的非经典大麻素及其药物组合物，其包含作为活性成分的新型（+）＆amp;蒎烯衍生物，其可用于预防和治疗自身免疫性疾病，包括 但不限于类风湿性关节炎，多发性硬化症，系统性红斑狼疮，重症肌无力，I型糖尿病，肝炎，牛皮癣，器官移植中的组织排斥，吸烟综合征如乳糜泻，肺部疾病如哮喘和Sjögren综合征，炎症包括 炎症性肠病，包括外周，内脏，神经性嗜酸性炎症和所谓疼痛，肌肉痉挛状态，包括心律失常，高血压和心肌缺血的心血管疾病，包括中风，偏头痛和丛集性头痛的神经障碍，包括帕金森病，阿尔茨海默氏症的神经变性疾病， 疾病，肌萎缩性侧索硬化，亨廷顿氏舞蹈病，朊病毒相关神经变性，CNS中毒和某些类型的癌症。

公开(公告)号：WO2003059855A1

公开(公告)日：2003-07-24

申请号：PCT/US2002/040885

申请日：2002-12-20

申请人： ARIZONA BOARD OF REGENTS ,  PETIT, George, R. ,  MOSER, Bryan, R.

发明人： PETIT, George, R. ,  MOSER, Bryan, R.

IPC分类号： C07C41/06

CPC分类号： C07F9/65517 ,  C07C43/23 ,  C07F9/12 ,  Y02P20/55

摘要： The original synthesis of combretastatin A-2 (1a) was modified to provide an efficient scale-up procedure for obtaining this antineoplastic stilbene. Subsequent conversion to a useful prodrug was accomplished by phosphorylation employing in situ formation of dibenzylchlorophosphite followed 30 by cleavage of the benzyl ester protective groups with bromotrimethylsilane to afford phosphoric acid intermediate 11. The latter was immediately treated with sodium methoxide to complete a practical route to the disodium phosphate prodrug (2a). The phosphoric acid precursor (11) of phosphate 2a was employed in a parallel series of reactions to produce a selection of metal and ammonium cation prodrug candidates. Each of the phosphate salts (2a-q) was evaluated with respect to relative solubility behavior, cancer cell growth inhibition, and antimicrobial activity.

摘要翻译： 改变了考布他汀A-2（1a）的原始合成，为获得这种抗肿瘤的二苯乙烯提供了有效的放大方法。 随后转化为有用的前体药物是通过使用原位形成二氯苄基亚磷酸酯进行磷酸化，然后通过用溴代三甲基甲硅烷裂解苄酯保护基来提供磷酸中间体11来完成的。后者立即用甲醇钠处理以完成实际路线 磷酸二钠前药（2a）。 磷酸二烷基酯（11）以平行的一系列反应方式使用，以产生金属和铵阳离子前体药物候选物的选择。 关于相对溶解行为，癌细胞生长抑制和抗微生物活性来评价磷酸盐（2a-q）中的每一种。

公开(公告)号：WO2003053932A1

公开(公告)日：2003-07-03

申请号：PCT/JP2002/013341

申请日：2002-12-20

申请人： 小池 透 ,  鈴木 正樹 ,  塩谷 光彦

发明人： 小池 透 ,  鈴木 正樹 ,  塩谷 光彦

IPC分类号： C07D213/36

CPC分类号： C07F9/6596 ,  C07F3/003 ,  C07F9/12

摘要： Zinc complexes capable of scavenging substances bearing anionic substituents, which are represented by the general formula (I-0): (I-0) wherein R's may be the same or different from each another and are each H; alkyl having 1 to 16 carbon atoms; acyl, carboxyalkyl, acylalkyl, carbamoylalkyl, cyanoalkyl, hydroxyalkyl, amino- alkyl, or haloalkyl (wherein each alkyl moiety has 1 to 16 carbon atoms); carboxyl; carbamoyl; hydroxyl; cyano; amino; or halogeno (with the proviso that the case wherein all of R's are H is excepted).

摘要翻译： 能够清除含有阴离子取代基的物质的锌络合物，其由通式（I-0）表示：（I-0）其中R可以彼此相同或不同，并且各自为H; 具有1至16个碳原子的烷基; 酰基，羧基烷基，酰基烷基，氨基甲酰基烷基，氰基烷基，羟基烷基，氨基 - 烷基或卤代烷基（其中每个烷基部分具有1至16个碳原子）; 羧基; 氨基甲酰基; 羟; 氰基; 氨基; 或卤素（条件是其中R全部为H的情况除外）。

公开(公告)号：WO02055526A1

公开(公告)日：2002-07-18

申请号：PCT/EP2001/015350

申请日：2001-12-28

IPC分类号： C09K21/12 ,  C07F9/12 ,  C08G79/04 ,  C08K5/51 ,  C08K5/523 ,  C08L85/02 ,  C08L101/00

CPC分类号： C07F9/12 ,  C08K5/523 ,  C08L69/00

摘要： The invention relates to the oligophosphates of the general formula (I), wherein R and R independently represent, individually selectable for every X, hydrogen, halogen, halogen-substituted or halogen-unsubstituted alkyl, alkyl, cycloalkyl, aryl having 1 to 20 carbon atom each, or R and R together with the carbon atom X to which they are bound form the structure of the formula (II) or a cylocalkyl structure substituted or not substituted by halogen, or R or R , on the carbon atom X, also form, together with an R or R on a further carbon atom X', a cyclic structure that is substituted or not substituted by halogen, R to R independently are the same or different and may represent an alkyl having 1 to 10 carbon atoms or halogen, X represents carbon, m is an integer of from 4 to 7, n is an integer of from 1 to 30, y is 0 or 1, and q may independently be the same or different and represent an integer of from 0 to 5. When used in thermoplastic compositions, said oligophosphates have excellent flame-retarding properties, improved thermal stability, a good viscosity level and excellent flowability.

摘要翻译： 通式低聚磷酸酯（I）：其中，R <1>和R <2>单独选择每个X，彼此独立地为氢，卤素，卤素取代或未取代的烷基，烷基，环烷基，芳基，在每种情况下具有1至20个碳原子的 可能，或者R <1>和R <2>一起与碳原子X与它们所连接的形式的式的结构（II）：以形成，或卤素 - 取代的或未取代的环结构，或者R <1>或R < 2>的碳原子X，带有R <1“>或R <2”>在另一个碳原子X“一起为环状卤素取代的或未取代的结构，R <3>至R <8>是彼此独立的每个，或 是不同的，并且碳原子数为1〜10的烷基或囟素可以是指X是碳m是从4到7的整数，n是从1到30的整数，y是0或1，q彼此独立地相同或不同的整数的 是从0至5 n可以在具有改进的耐热性，良好的韧性水平和优异的流动性的热塑性组合物表现出良好的阻燃性。

公开(公告)号：WO02009686A2

公开(公告)日：2002-02-07

申请号：PCT/FR2001/002443

申请日：2001-07-26

IPC分类号： C07D295/12 ,  A61K31/04 ,  A61K31/137 ,  A61K31/166 ,  A61K31/18 ,  A61K31/222 ,  A61K31/24 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/445 ,  A61K31/495 ,  A61K31/63 ,  A61K31/661 ,  A61K31/6615 ,  A61P17/14 ,  A61P21/00 ,  A61P25/00 ,  A61P25/28 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P43/00 ,  C07C69/157 ,  C07C211/53 ,  C07C215/78 ,  C07C215/80 ,  C07C217/84 ,  C07C229/36 ,  C07C235/66 ,  C07C303/38 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/37 ,  C07D211/96 ,  C07D233/84 ,  C07D241/04 ,  C07D295/135 ,  C07D295/155 ,  C07D295/192 ,  C07D295/26 ,  C07D333/22 ,  C07D333/34 ,  C07D333/38 ,  C07F9/12

CPC分类号： C07D295/26 ,  A61K31/137 ,  A61K31/165 ,  A61K31/18 ,  A61K31/381 ,  A61K31/445 ,  A61K31/495 ,  A61K31/63 ,  C07C217/84 ,  C07C229/36 ,  C07C235/66 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/37 ,  C07D233/84 ,  C07D295/135 ,  C07D295/192 ,  C07D333/22 ,  C07D333/34 ,  C07F9/12

摘要： The invention concerns novel cdc25 phosphatase inhibitors, and in particular cdc25-C, which correspond to the general formula (I) wherein: A represents a carbocyclic aryl radical optionally substituted 1 to 3 times by one or more radicals independently selected among a halogen atom and an alkyl, hydroxy, alkoxy, alkylthio or NR R radical wherein R and R represent a hydrogen atom or an alkyl radical or R and R form together with the nitrogen atom a heterocycle of 4 to 7 members comprising 1 to 2 heteroatoms, the members required to complete the heterocycle being selected independently among the CR R -, -O-, -S and NR - radicals, R and R representing independently each time they are involved a hydrogen atom or an alkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino radical, and R5 representing independently each time it is involved a hydrogen atom or an alkyl radical, or A represents a phenyl radical substituted by a phenyl radical optionally substituted 1 to 3 times by one or more radicals selected independently among a halogen atom and an alkyl, hydroxy, alkoxy, alkylthio or NR R radical wherein R and R represent a hydrogen atom or an alkyl radical; B represents a -(CH2)i-(CO)- or -NH-CO-(CH2)n or -(CH2)p and i and n being integers from 0 to 2 and p being an integer from 0 to 1; W represents a hydrogen atom or an alkyl radical; X represents a -(CH2)q- or (CH2)j-CO-(CH2)r-, q being an integer from 1 to 4 and j and r being integers from 0 to 6; Y represents in particular a nitrophenyl, aminophenyl, alkylaminophenyl or dialkylaminophenyl radical or the radical (T).

摘要翻译： 本发明涉及新的cdc25磷酸酶抑制剂，特别是对应于通式（I）的cdc25-C，其中：A代表一个或多个独立地选自卤原子和 烷基，羟基，烷氧基，烷硫基或NR 1 R 2基团，其中R 1和R 2表示氢原子或烷基或R 1和R 2与 氮原子，含有1至2个杂原子的4至7个成员的杂环，完成杂环所需的成员独立地选自CR 3 - ， - O - ， - S和NR 5 - 基团 R 3和R 4每次涉及氢原子或烷基，羟基，烷氧基，氨基，烷基氨基或二烷基氨基时独立地表示，并且R 5独立地表示每次涉及氢原子或烷基 或者A表示被任选取代的苯基取代的苯基 在卤素原子和烷基，羟基，烷氧基，烷硫基或NR 1 R 2基团中独立选择的一个或多个基团，其中R 1和R 2表示氢原子或 烷基; B表示 - （CH2）i-（CO） - 或-NH-CO-（CH2）n或 - （CH2）p，i和n为0至2的整数，p为0至1的整数; W表示氢原子或烷基; X表示 - （CH 2）q - 或（CH 2）j -CO-（CH 2）r - ，q为1至4的整数，j和r为0至6的整数; Y特别表示硝基苯基，氨基苯基，烷基氨基苯基或二烷基氨基苯基或基团（T）。