| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 用于治疗代谢性疾病的化合物、药物组合物和方法 | CN200580012709.2 | 2005-02-24 | CN1946666A | 2007-04-11 | M·阿克曼; J·乌泽; D·C·H·林; 刘纪文; 罗健; J·C·马蒂纳; W·邱; J·D·里根; M·J·施米特; 王英才; R·沙尔马; S·J·沙特尔沃斯; 孙莹; J·张; L·朱; 刘进前; 马治华 |
| 本发明提供用于例如调控受治疗者胰岛素水平的化合物，该化合物具有通式：Q－L1－P－L2－M－X－L3－A，其中变量Q、L1、P、L2、M、X、L3和A在说明书中提供。本发明还提供使用该化合物治疗例如II型糖尿病的组合物和方法。 | ||||||
| 2 | 制备旋光2-芳基链烷酸，特别是2-芳基丙酸的方法 | CN90103564.5 | 1990-05-16 | CN1050373A | 1991-04-03 | 海瑞茨·H·普拉地斯; 萨米尔·B·汉那; 伯恩德·斯程内德 |
| 这里揭示的是用立体有择化学方法制备具有通式I的药物活性化合物和它们的生理耐受盐及其酯的方法，式中R和Ar定义详见说明书，该方法包括：a)在还原剂和有机溶剂存在下，将式(I′)的羰基底物与立体有择试剂反应，生成对映体甲醇，和b)使得到的对映体甲醇反应得到最终产物。 | ||||||
| 3 | 用于降低尿酸的化合物和方法 | CN200980108707.1 | 2009-03-13 | CN101969773B | 2015-08-19 | 詹姆斯·邓恩·奥尼尔; 迈克尔·K·巴纳特; 里德·W·冯博斯特尔; 沙林·夏尔马; 拉马钱德兰·阿鲁德钱德兰 |
| 通过施用式(I)化合物或其药学可接受的盐降低了哺乳动物对象的尿酸并增大其尿酸排泄。式(I)中，m为0、1、2、3或4；n为0或1；m+n不大于4；t为0或1；q为0或1；r为0、1或2。R6是氢、甲基或乙基且R12是氢或甲基，或者R6是羟基且R12是氢，或者R6是O且R12不存在，或者R6和R12连起来是-CH2CH2-。R7是氢或具有1～3个碳原子的烷基。R8和R9其中之一是具有1～3个碳原子的烷基，而另一个是氢或具有1～3个碳原子的烷基。R10是氢、卤素、具有1～3个碳原子的烷基或具有1～3个碳原子的烷氧基。X是C(O)，r为0，t为0；或X是NH(R11)，其中R11是氢或具有1～3个碳原子的烷基。A是不具有取代基的苯基或者是具有选自下述基团中的1个或2个基团作为取代基的苯基：卤素、羟基、甲基、乙基、全氟甲基、甲氧基、乙氧基和全氟甲氧基；或者A是具有1或2个选自N、S和O的环杂原子的五元或六元杂芳环，所述杂芳环通过环碳与式I的化合物的剩余部分共价连接；或者A是具有3～6个环碳原子的环烷基，其中所述环烷基不具有取代基或者一个或两个环碳独立地被甲基或乙基单取代。具有降尿酸效果的式(I)化合物用来治疗或预防各种疾病，包括痛风、高尿酸血症、不满足通常证明为高尿酸血症诊断的水平的尿酸水平的升高、肾功能障碍、肾结石、心血管疾病、发展心血管疾病的风险和认知障碍。所述式(I)为： | ||||||
| 4 | dl—萘普生的缩合醛肟合成法 | CN86100855 | 1986-02-01 | CN86100855B | 1988-07-13 | 丁福璋 |
| 一种ｄ１－萘普生合成方法，起始原料６－甲氧基萘乙酮经与异丙醇及氯乙酸异丙酯于４８～５３℃缩合，并于５０～７０℃成６－甲氧基萘丙醛，然后于７０～８０℃肟化。１２０～１３５℃脱氨而成ｄ１－萘普生，再调节ｐＨ值到所需要范围而精制成为ｄ１－萘普生精制品。用本发明的合成方法合成的产物得率达８８．８～９１．４％，产品成本下降一半，三废很少。 | ||||||
| 5 | 用于制备具有CGRP拮抗性质的N-哌啶基-苯并二氮杂的方法 | CN200780030188.2 | 2007-08-16 | CN101600705A | 2009-12-09 | 冈瑟·赫克勒; 沃纳·拉尔; 尤维·里斯 |
| 本发明涉及一种制备通式(I)化合物、其可药用盐和溶剂合物的方法，其中R1及R2如权利要求1中所定义，所述的物质可由通式(II)化合物起始制备；其中R1如权利要求1中所定义。 | ||||||
| 6 | 作为PPAR调节剂的化合物和组合物 | CN200580019645.9 | 2005-05-13 | CN1980894A | 2007-06-13 | R·埃波; M·阿奇米奥拉 |
| 本发明提供了化合物、包含这类化合物的药物组合物和使用这类化合物来治疗或预防与过氧化物酶体增殖物激活受体(PPAR)家族活性、特别是PPARδ活性有关的疾病或疾患的方法。 | ||||||
| 7 | 原油脱酸工艺方法 | CN200410091495.X | 2004-11-26 | CN1632068A | 2005-06-29 | 李世洪; 张志川 |
| 本发明涉及一种常温条件下，采用化学处理剂进行原油脱酸工艺方法。特征是：(a)用脱酸剂水溶液加入原油体系中，以使原油体系中有机酸转入水相中；(b)提取水相沉淀，上层为环烷酸层，下层为富含脱酸剂的水层；(c)提取水层加入活化剂，脱酸剂恢复活性，上层为脱酸剂层，下层为污水层，上层脱酸剂重复使用，下层污水达到排放标准。本发明在常温下处理原油，不需要特殊设备。处理后原油总酸值降低到0.5mgKOH/g以下。其次，提取有工业价值的环烷酸。第三，使脱酸剂得到回收，重复使用。第四，废水能达到排放标准。 | ||||||
| 8 | 新的3－芳基丙酸衍生物和其类似物 | CN99809354.8 | 1999-05-31 | CN1312795A | 2001-09-12 | K·安德松; M·波伊杰; J·戈特弗里斯; T·因格哈德特; L·李; E·-L·林德斯特德特-阿尔斯特马克 |
| 通式(Ⅰ)所示新的3－芳基丙酸衍生物和其类似物,其立体异构体和旋光异构体以及外消旋体,和其可药用盐、溶剂化物以及结晶形式,所述化合物的制备方法,含有所述化合物的药物制剂,以及所述化合物在与胰岛素抗性有关的临床病症中的应用。 | ||||||
| 9 | SÍNTESIS DE ANALOGOS DE Y-AMINOÁCIDOS Y PRODUCTOS OBTENIDOS | PCT/MX2015/000081 | 2015-05-28 | WO2015183067A1 | 2015-12-03 | FERNÁNDEZ ZERTUCHE, Mario; TOVAR GUDIÑO, Erika; TRUJILLO FERRARA, José Guadalupe; GUEVARA SALAZAR, Juan Alberto |
La presente invención se refiere a compuesto de Fórmula (Ver Fórmula) que son útiles como fármacos en el tratamiento de transtornos neurodegenerativos crónicos de tipo del mal de Huntington, Parkinson y Epilepsia, entre otros. La invención también se refiere a novedosos métodos para la síntesis de dichos análogos y sus sales y solvatos farmacéuticamente aceptable. |
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| 10 | PKC-EPSILON ACTIVATOR | US13885751 | 2011-11-15 | US20130331454A1 | 2013-12-12 | Tomoyuki Nishizaki; Akito Tanaka |
| The present invention aims to obtain an optical isomer of DCP-LA, which shows more superior activity and is suitable for clinical utilization, and provide an agent having a superior PKC-ε activation action, a prophylactic and/or therapeutic agent for neurotransmitter release disorders, and a prophylactic and/or therapeutic agent for neuropsychiatric diseases, which contain the isomer as an active ingredient.A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and a selective PKC-ε activator containing same as an active ingredient, and is the like. | ||||||
| 11 | Process for the preparation of optically active alpha-arylalkanoic acids and novel intermediates thereof | US82196 | 1987-08-05 | US4888433A | 1989-12-19 | Claudio Giordano; Graziano Castaldi; Fulvio Uggeri; Silvia Cavicchioli |
| A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions. The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids. | ||||||
| 12 | Diphenylmethane compounds | US474729 | 1983-03-10 | US4564685A | 1986-01-14 | John W. A. Findlay; Geoffrey G. Coker |
| This disclosure describes compounds of Formula I. ##STR1## (including their pharmaceutically acceptable salts and esters) which have potent antihistamine activity which are substantially free from sedative effects. | ||||||
| 13 | Nucleophilic substitution process | US317321 | 1981-11-02 | US4370278A | 1983-01-25 | Barbara C. Stahly; G. P. Stahly |
| 2-(Fluoronitrobenzene)alkyl cyanides are prepared by reacting a fluoronitrobenzene with an alpha-substituted alkyl cyanide in a substantially anhydrous aprotic solvent and in the presence of a base so that the alkyl cyanide reactant undergoes a nucleophilic substitution reaction on an unsubstituted carbon atom of the fluoronitrobenzene during which the alpha-substituent of the alkyl cyanide reactant functions as a leaving group. Use of 2-fluoronitrobenzene and an alpha-substituted propionitrile (e.g., 2-chloropropionitrile) produces a novel compound, 2-(3-fluoro-4-nitrobenzene)propionitrile. Reduction of the nitro substituent produces another novel compound, 2-(4-amino-3-fluorobenzene)proprionitrile. This can readily be converted to 2-(3-fluoro-4-biphenylyl)propionitrile by means of a Gomberg-Bachmann reaction with an aromatic hydrocarbon or substituted aromatic hydrocarbon which in turn can be converted on hydrolysis into the corresponding 2-(2-fluoro-4-biphenylyl)propionic acid. Use of benzene in the Gomberg-Bachmann reaction thus enables production of flurbiprofen, a well-known pharmaceutical. | ||||||
| 14 | Process for preparing aromatic acetic acid | US93818 | 1979-11-13 | US4268442A | 1981-05-19 | Kiyosi Kondo; Tamotsu Fujimoto; Minoru Suda; Daiei Tunemoto |
| There are disclosed processes for preparing an aromatic acetic acid by the reaction of an aromatic aldehyde with a combination of a trihalomethane and an alkanethiol, and by the reaction of an alcohol derivative (2,2,2-trihalo-1-arylethanol) with an alkanethiol, in the presence of a base in a mixed medium of water and an aprotic polar solvent. | ||||||
| 15 | PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES | US13401459 | 2012-02-21 | US20120149768A1 | 2012-06-14 | Thomas J. Nelson; Daniel L. Alkon |
| The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. | ||||||
| 16 | METHOD FOR PREPARING ACTIVATED ESTERS | US13140254 | 2009-12-15 | US20110313168A1 | 2011-12-22 | Antony Bigot |
| The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P2 is precipitated. The invention also relates to products of the formula P1. | ||||||
| 17 | Process for preparing optically active 2-aryl-alkanoic acids, in particular 2-aryl-propionic acids | US524377 | 1990-05-16 | US5380927A | 1995-01-10 | Henrich H. Paradies; Samir B. Hanna; Bernd Schneider |
| A chemical process is disclosed for the preparation of a pharmaceutically active compound in stereospecific form selected from the group of compounds having the formula: ##STR1## and their physiologically compatible salts and esters, wherein R is a lower alkyl and Ar a monocyclic, polycyclic or orthocondensed polycyclic aromatic group having up to 12 carbon atoms in the aromatic ring, and which may be substituted or unsubstituted in the aromatic ring, comprising the steps:a) reacting a carbonyl substrate of the formula: ##STR2## where R and Ar have the meanings given above, with a stereospecific reagent in the presence of a reducing agent and an organic solvent to form the enatiomeric carbinol andb) reacting the enantiomeric carbinol obtained to form the end product. | ||||||
| 18 | Leukotriene antagonists | US37284 | 1987-04-10 | US4874777A | 1989-10-17 | F. Patrick Carr; Robert D. Dillard; Doris E. McCullough |
| This invention provides benzene derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes. | ||||||
| 19 | Optically active ketals, processes for their preparation and their use in the synthesis of alpha-arylalkanoic acids | US134197 | 1987-12-17 | US4855464A | 1989-08-08 | Claudio Giordano; Graziano Castaldi; Fulvio Uggeri; Silvia Cavicchioli |
| Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.4) alkyl group;X represents a chlorine, bromine or iodine atom, an hydroxy, acyloxy, alkylsulphonyloxy or arylsulphonyloxy group;the carbon atoms marked by an asterisk are both contemporaneously in the R or S configuration, are described.The preparation of the compound of formula I by ketalization or by trans-ketalization with tartaric acid derivatives and their rearrangement into alpha-arylalkanoic acids is decribed too. | ||||||
| 20 | 1,1-Diaminoalkane derived sweeteners | US503853 | 1983-06-13 | US4571345A | 1986-02-18 | Michael S. Verlander; William D. Fuller; Murray Goodman |
| Compounds of the formula: ##STR1## wherein n is 0 or 1, R is lower alkyl (substituted or unsubstituted), R' is H or lower alkyl, and R" is a branched alkyl, alkyl-cycloalkyl, cycloalkyl, polycycloalkyl (poly=2 or more, fused or non-fused), phenyl or alkyl-substituted phenyl, and physiologically acceptable cationic and acid addition salts thereof, which compounds are potent sweeteners. These derivatives of gem-diaminoalkanes are many times sweeter than sugar and are free from undesirable flavor qualities. Furthermore, they possess an unanticipated high degree of solubility compared with known synthetic sweeteners. In addition, the compounds possess high stability so that they can be used in all types of beverages and in conventional food processing. Sweetening compositions and sweetened edible compositions of these compounds are also provided. | ||||||
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