| 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 | α-氟代查耳酮类衍生物及其应用 | CN202011323949.7 | 2020-11-23 | CN112824380A | 2021-05-21 | 楼金芳; 冯恩光; 沈锡明 |
| 本发明提供一种α‑氟代查耳酮类衍生物及其应用，所述衍生物包括其药学上可接受的盐。本发明还提供了一种所述衍生物及其药学上可接受的盐在制备治疗PPAR受体相关病症的药物中应用。本发明提供的衍生物体内吸收好，具有生物利用度高、药效作用强的特点，因此有巨大的临床应用价值。 | ||||||
| 2 | 一种反式-1,3-二羟基环丁烷-1-羧酸的制备方法 | CN201811007287.5 | 2018-08-31 | CN109096098B | 2021-04-23 | 练华文; 刘贵华 |
| 本发明公开了一种反式‑1,3‑二羟基环丁烷‑1‑羧酸的制备方法，主要解决反式1,3‑二羟基环丁烷‑1‑羧酸合成工艺缺乏的技术问题，包括以下步骤：以化合物II(3‑(苄氧基)‑1‑环丁酮)为原料，与三甲基氰硅烷反应生成化合物III；化合物III的氰基经过醇解后生成化合物IV；再水解生成化合物V；化合物V经过重结晶分离得到顺式化合物VI；化合物VI经过酯化后生成化合物VII；化合物VII中羟基经过叔丁基二甲基氯硅烷保护后生成化合物VIII；化合物VIII经过脱苄基保护基得到化合物IX；化合物IX与对硝基苯甲酸经过Mitsunobu反应生成化合物X，再脱去对硝基苯甲酰基得到化合物XI，羟基构型发生了翻转；最后水解得到化合物I(反式‑1,3‑二羟基环丁烷‑1‑羧酸)。 | ||||||
| 3 | 吉卡宾、其药学上可接受的盐、其组合物和其使用方法 | CN201980084618.1 | 2019-10-17 | CN113396138A | 2021-09-14 | D·C·安尼丘; C·L·比斯盖尔; M·B·格林 |
| 本发明提供了包含吉卡宾钙盐水合物晶型2或C3的片剂，所述晶型各自具有如通过激光衍射测得在35μm至90μm的范围内的PSD90，并且其中所述片剂具有以在37℃±0.5℃于pH 5.0乙酸钾缓冲液中在不超过45分钟内至少80％的溶出曲线为特征的吉卡宾溶出曲线，如通过使用216nm至230nm检测的UV‑Vis吸收所测量。本发明进一步提供了吉卡宾钙盐水合物晶型4、5和6。所述片剂和吉卡宾钙盐水合物晶型4、5和6可用于治疗或预防肝脏疾病或异常肝脏疾患、脂蛋白或葡萄糖代谢障碍、心血管或相关血管病症、由纤维化引起的疾病(例如肝纤维化)或与炎症相关的疾病(例如肝脏炎症)。 | ||||||
| 4 | 一种反式-1,3-二羟基环丁烷-1-羧酸的制备方法 | CN201811007287.5 | 2018-08-31 | CN109096098A | 2018-12-28 | 练华文; 刘贵华 |
| 本发明公开了一种反式-1,3-二羟基环丁烷-1-羧酸的制备方法，主要解决反式1,3-二羟基环丁烷-1-羧酸合成工艺缺乏的技术问题，包括以下步骤：以化合物II(3-(苄氧基)-1-环丁酮)为原料，与三甲基氰硅烷反应生成化合物III；化合物III的氰基经过醇解后生成化合物IV；再水解生成化合物V；化合物V经过重结晶分离得到顺式化合物VI；化合物VI经过酯化后生成化合物VII；化合物VII中羟基经过叔丁基二甲基氯硅烷保护后生成化合物VIII；化合物VIII经过脱苄基保护基得到化合物IX；化合物IX与对硝基苯甲酸经过Mitsunobu反应生成化合物X，再脱去对硝基苯甲酰基得到化合物XI，羟基构型发生了翻转；最后水解得到化合物I(反式-1,3-二羟基环丁烷-1-羧酸)。 | ||||||
| 5 | 5-Halovinyl-2'-deoxyuridine derivatives | EP83305456 | 1983-09-16 | EP0104066A3 | 1984-06-06 | Scopes, David Ian Carter; Newton, Roger Frank; Ravenscroft, Paul; Cookson, Richard Clive |
Compounds of general formula (I):
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| 6 | Triazolylmethyl-cyclopropyl-Derivate | EP90123613.3 | 1990-12-08 | EP0438686A3 | 1991-12-11 | Scherkenbeck, Jürgen, Dr.; Stroech, Klaus, Dr.; Fugmann, Burghard, Dr.; Dutzmann, Stefan, Dr. |
Triazolylmethyl-cyclopropyl-Derivate der Formel
Neue Zwischenprodukte, Verfahren zu deren Herstellung und deren Verwendung zur Synthese von Triazolylmethyl-cyclopropyl-Derivaten der Formel (I). |
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| 7 | GEMCABENE, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR | PCT/US2019/056769 | 2019-10-17 | WO2020081837A1 | 2020-04-23 | ONICIU, Daniela Carmen; BISGAIER, Charles Larry; GREENE, Matthew Benjamin |
This invention provides tablets comprising gemcabene calcium salt hydrate Crystal Forms 2 or C3, each having a PSD90 ranging from 35 urn to 90 urn as measured by laser light diffraction and wherein the tablet has a gemcabene dissolution profile characterized by a percent dissolution profile of at least 80 in pH 5.0 potassium acetate buffer at 37 C +- 0.5 C in no more than 45 minutes as measured by UV-Vis absorption using a detection of 216 nm to 230 nm. This invention further provides gemcabene calcium salt hydrate Crystal Foms 4, 5 and 6. The tablets and gemcabene calcium salt hydrate Crystal Forms 4, 5 and 6 are useful for treating or preventing liver disease or an abnormal liver condition, a disorder of lipoprotein or glucose metabolism, a cardiovascular or related vascular disorder, a disease caused by fibrosis (such as liver fibrosist or a disease associated with inflammation (such as liver inflammation). |
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| 8 | NOVEL CYCLOBUTANE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME | PCT/JP1998/002206 | 1998-05-20 | WO98052930A1 | 1998-11-26 | |
| A process for producing cyclobutane derivatives useful as intermediates for cyclobutanenucleoside derivatives and the like useful as an antiviral agent; the novel intermediates; and a method for optical resolution. The cyclobutane derivatives can be efficiently produced under practical conditions. Optically active intermediates can be easily obtained. (a) The process is charecterized by using a magnesium-base Lewis acid as a catalyst in the production of a cyclobutane derivative through a [2+2] cycloaddition reaction shown by reaction scheme (I) (e.g., the condensation of a fumaric ester with a ketene derivative) wherein R<5> and R<6> each represents optionally substituted C1-20 linear, branched, or alicyclic alkyloxy (the substituents including (un)substituted phenyl) or a group represented by formula (4) (wherein A represents C2-5 alkylene; Y represents oxygen or sulfur; Z represents oxygen, sulfur, or -NR<0>-; and R<0> represents hydrogen or a substituent); B<1> and B<2> each represents oxygen or sulfur; R<4> represents hydrogen, C1-5 alkyl or alkoxy, or aralkyloxy; R<7> and R<8> each represents C1-5 alkyl, C7-10 aralkyl, or silyl, or represents C2-10 alkylene when R<7> and R<8> are bonded to each other to form a ring; R<5> and R<6>, B<1> and B<2>, and R<7> and R<8> each may be the same or different; and each double bond may be cis or trans. (b) In the optical resolution method, cyclobutanedicarboxylic acid derivatives derived from the cyclobutane derivatives or the like are optically resolved as salts thereof with an optionally substituted optically active N-benzyl-1-phenylethylamine. | ||||||
| 9 | PROCESS FOR THE PREPARATION OF FLUORINATED UNSATURATED COMPOUNDS AND PROCESS FOR THE PRODUCTION OF FLUOROPOLYMERS | PCT/JP2001/007496 | 2001-08-30 | WO02020445A1 | 2002-03-14 | |
| A process is provided by which fluorinated unsaturated compounds that were difficultly synthesizable or prepared by uneconomical synthesis processes can be prepared from inexpensive and easily available raw materials in a short step in high yield. Fluorinated unsaturated compounds (2): R |
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| 10 | PROCESS FOR PRODUCING A VIC-DICHLORO ACID FLUORIDE | PCT/JP2000/005888 | 2000-08-30 | WO01016085A1 | 2001-03-08 | |
The process for producing a vic-dichloro acid fluoride compound in a short process and in good yield from the starting material which is inexpensive and readily available is provided. (R-EH1-)CRCH2-OCOR |
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| 11 | Triazolylmethyl-cyclopropyl-Derivate | EP90123613.3 | 1990-12-08 | EP0438686A2 | 1991-07-31 | Scherkenbeck, Jürgen, Dr.; Stroech, Klaus, Dr.; Fugmann, Burghard, Dr.; Dutzmann, Stefan, Dr. |
Triazolylmethyl-cyclopropyl-Derivate der Formel
Neue Zwischenprodukte, Verfahren zu deren Herstellung und deren Verwendung zur Synthese von Triazolylmethyl-cyclopropyl-Derivaten der Formel (I). |
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| 12 | 5-Halovinyl-2'-deoxyuridine derivatives | EP83305456.2 | 1983-09-16 | EP0104066B1 | 1988-08-10 | Scopes, David Ian Carter; Newton, Roger Frank; Ravenscroft, Paul; Cookson, Richard Clive |
| 13 | 5-Halovinyl-2'-deoxyuridine derivatives | EP83305456.2 | 1983-09-16 | EP0104066A2 | 1984-03-28 | Scopes, David Ian Carter; Newton, Roger Frank; Ravenscroft, Paul; Cookson, Richard Clive |
Compounds of general formula (I):
|
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| 14 | GEMCABENE, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR | US17583081 | 2022-01-24 | US20220332672A1 | 2022-10-20 | Daniela Carmen ONICIU; Charles Larry BISGAIER; José Rui GOMES; Stefan HECKHOFF |
| This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 μm to about 90 μm, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia. | ||||||
| 15 | GEMCABENE, PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR | US16402853 | 2019-05-03 | US20200148617A1 | 2020-05-14 | Daniela Carmen ONICIU; Charles Larry BISGAIER; José Rui GOMES; Stefan HECKHOFF |
| This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 μm to about 90 μm, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia. | ||||||
| 16 | Process for making carboxyalkylates of branched alcohols | US10926222 | 2004-08-25 | US20060047168A1 | 2006-03-02 | Bijan Harichian; Jose Rosa; Victor De Florio |
| Process for carboxy-alkylation, particularly carboxymethylation, of branched alcohols includes the reaction of isoalcohols with potassium-t-butoxide or sodium-t-butoxide and with salt of halogenated alkanoic acid in the presence of the isoalcohol (starting alcohol) as the solvent. Produced are isoalcohol carboxy-alkylates (preferably, carboxymethylates) in excellent yields and purity. | ||||||
| 17 | Process for the preparation of alkylidenecyclopentanone derivatives | US11114538 | 2005-04-26 | US20050187299A1 | 2005-08-25 | Christian Chapuis; Hans Wuest |
| The present invention relates to the field of organic synthesis and more particularly to a new process for the preparation of a compound of formula (I), in the form of any one of its isomers or a mixture thereof, wherein, more preferably, G represents a C═O group, R1 represents a butyl group and R2 represents a methyl group. The process of the invention involves an 2-(1-hydroxyalkyl)-cyclopent-2-en-1-one derivative, as starting material, which can be then converted into a compound of formula (I) by a process comprising a thermal rearrangement. The 2-alkylidene-3-oxo-cyclopentylacetate derivative and the 2-(1-hydroxyalkyl)-cyclopent-2-en-1-one derivative are also an object of the invention. | ||||||
| 18 | Heterofunctional copolymers of glycerol and polyethylene glycol, their conjugates and compositions | US10926215 | 2004-08-25 | US20050048650A1 | 2005-03-03 | Francis Ignatious |
| The present invention relates to heterofunctional copolymers of glycerol and polyethylene glycol, conjugates of these heterofunctional copolymers with bioactive agents, nanoparticles, hydrophobic polymers and/or lipids; and to compositions containing these conjugates. | ||||||
| 19 | Preparation of halogenated compounds | US281809 | 1994-07-28 | US5504248A | 1996-04-02 | Paul J. Krusic; Zhen-Yu Yang |
| Halogenated compounds are prepared by ring opening reactions of highly fluorinated cyclopropanes with chlorine, bromine, iodine, or mixtures thereof at temperatures over 100.degree. C. A novel compound, which is one type of compound produced, is a highly fluorinated and halogenated ether and other novel compounds are starting materials or products. The products of the process are useful as chain transfer agents for certain free radical polymerizations, and as chemical intermediates in the preparation of various products such as surfactants and textile surface treatments. | ||||||
| 20 | Naphthoquinone derivatives | US456052 | 1989-12-26 | US5053432A | 1991-10-01 | Alan T. Hudson; Anthony W. Randall |
| Novel antiprotozoal naphthoquinones having the general formula ##STR1## (wherein either R.sup.1 is hydrogen and R.sup.2 is selected from C.sub.1-6 alkoxy, aralkoxy, C.sub.1-6 alkyl-C.sub.1-6 alkoxy, phenyl substituted by one or two groups selected from halogen and C.sub.1-6 alkyl, halogen and perhalo-C.sub.1-6 alkyl; or R.sup.1 and R.sup.2 are both C.sub.1-6 alkyl or phenyl; and n is 0 or 1) and salt thereof. The compounds of formula (I) are useful for the treatment or prophylaxis of protozoal diseases including malaria, theileriosis and coccidiosis. Various processes for preparing compounds of formula (I) are described. | ||||||
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