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1. 发明申请

WO2021245671A1 CANNABIDIOLIC ACID (CBDA) DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：WO2021245671A1
公开(公告)日：2021-12-09
申请号：PCT/IL2021/050661
申请日：2021-06-03
申请人： EPM (IP), INC. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
发明人： SWISA, Reshef , IOSUB-AMIR, Anat , SHAHARABANI, Ron , MECHOULAM, Raphael , KOGAN, Natalya M.
IPC分类号： C07C69/92 , C07C65/28 , C07C65/26 , C07C65/21 , A61K31/192 , A61K31/216 , A61K36/185 , A61P1/00 , A61P1/08 , A61P1/16 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P13/12 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P27/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00
摘要： The present invention provides novel compounds comprising cannabidiolic acid (CBDA) derivatives, including acids and esters, and uses thereof in the treatment of various diseases, disorders, conditions and symptoms.

3. 发明申请

WO2008080992A3 A PROCESS FOR THE PREPARATION OF 6-[3-(1-ADAMANTYL)-4-METHOXYPHENYL-2-NAPHTOIC ACID 审中-公开
标题翻译：制备6- [3-（1-氨基）-4-甲氧基苯基-2-萘酸的方法
公开(公告)号：WO2008080992A3
公开(公告)日：2008-09-18
申请号：PCT/EP2007064647
申请日：2007-12-28
申请人： KALVINSH IVARS , CHERNOBROVIJS ALEKSANDRS , TRIBULOVICH VYACHESLAV , LABEISH VLADIMIR
发明人： KALVINSH IVARS , CHERNOBROVIJS ALEKSANDRS , TRIBULOVICH VYACHESLAV , LABEISH VLADIMIR
IPC分类号： C07C51/09 , C07C65/26 , C07C67/343 , C07C69/00 , C07F5/02
CPC分类号： C07C67/343 , C07C51/09 , C07C2603/74 , C07C65/26 , C07C69/94
摘要： A process for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid from 2-(1-adamantyl)-4-bromanisolee is disclosed, based on transformation of 2-(1-adamantyl)-4-bromanisole into a Grignard's reagent by using metallic magnesium, anhydrous lithium chloride and dibromoethane followed by transmetallation with borates to 3-(adamantyl)-4-methoxyphenylboronic acid, wich is converted into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid esters by Suzuki-Miyaura cross-coupling reaction with alkyl-6-halonaftoates catalyzed by Pd [0] or Pd/phosphine ligands and followed by basic hydrolysis in ethylene glycol or 1,2-propanediol of ester thus obtained into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid.
摘要翻译：公开了从2-（1-金刚烷基）-4-溴苯甲醚制备6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸的方法，基于2-（1-金刚烷基））-4-溴苯甲醚通过使用金属镁，无水氯化锂和二溴乙烷转化成格利雅试剂，然后与硼酸盐转化成3-（金刚烷基）-4-甲氧基苯基硼酸，转化为6- [3-（1-金刚烷基） -4-甲氧基苯基] -2-萘甲酸酯，通过Suzuki-Miyaura交叉偶联反应与Pd [0]或Pd /膦配体催化的烷基-6-卤代沸石反应，随后在乙二醇或1,2-丙二醇中碱性水解的酯，由此得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸。

4. 发明申请

WO2007125542A3 A PROCESS FOR PREPARATION OF ADAPALENE 审中-公开
标题翻译：一种制备ADAPALENEN的方法
公开(公告)号：WO2007125542A3
公开(公告)日：2007-12-27
申请号：PCT/IN2007000145
申请日：2007-04-09
申请人： USV LTD , TARUR RADHAKRISHNAN VENKATASUB , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , PATNEKAR SUBODH SHASHIKANT , PATIL SACHIN SHIVAJI
发明人： TARUR RADHAKRISHNAN VENKATASUB , BHISE NANDU BABAN , SATHE DHANANJAY GOVIND , PATNEKAR SUBODH SHASHIKANT , PATIL SACHIN SHIVAJI
IPC分类号： A61K31/192 , A61P17/10 , C07C41/16 , C07C43/225 , C07C51/09 , C07C65/26 , C07C67/343
CPC分类号： C07C67/343 , C07C41/16 , C07C51/09 , C07C51/412 , C07C2603/74 , C07C65/26 , C07C69/94 , C07C43/225
摘要： The present invention discloses a process for preparation of highly pure Adapalene, chemically designated as 6-[3-(l-adamantyl)-4-methoxy phenyl]-2-naphthoic acid (I) comprising: a) reacting 1-adamantanol with 4-bromophenol (II) in presence of sulphonic acid with or without the use of organic solvent to give 2-(l-adamantyl)-4- bromophenol (III); b) alkylating compound of formula(III) with dimethylsulphate in presence of base in organic solvent to obtain 2-(l-adamantyl)-4-bromoanisole (IV); c) C-C coupling the compound of formula (IV) with methyl-6-bromo-2- naphthoate using magnesium, purified zinc chloride and NiCl 2 -DPPE in THF at a temperature of 40-60°C tO obtain methyl ester of 6-[3-(l- adamantyl)-4-methoxy phenyl] -2-naphthoic acid (V); d) purifying crude methyl ester of 6-[3-(l-adamantyl)-4-methoxy phenyl]-2- naphthoic acid (V) using a mixture of organic solvent to obtain pure compound (V); e) hydrolyzing the compound (V) with a solution of alkali in organic solvent to obtain metal salt of 6-[3-(l-adamantyl)-4-methoxy phenyl] -2-naphthoic acid (VI); f) acidifying metal salt of adapalene (VI) using organic or inorganic acid to obtain crude adapalene (I) and g) recrystallizing the crude adapalene (I) using a mixture of organic solvents to obtain pure adapalene (I).
摘要翻译：本发明公开了一种制备高纯度阿达帕林的方法，化学名为6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（I），其包括：a）使1-金刚烷醇与4 （II）在有或没有使用有机溶剂的情况下在磺酸存在下反应，得到2-（1-金刚烷基）-4-溴酚（III）; b）在碱的存在下，在有机溶剂中，用式（III）的化合物与硫酸二甲酯烷基化，得到2-（1-金刚烷基）-4-溴苯甲醚（Ⅳ）; c）在40-60℃的温度下，使用镁，纯化氯化锌和NiCl 2 -DPPE在THF中将式（Ⅳ）化合物与6-溴-2-萘甲酸甲酯偶联，得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的甲酯。 d）使用有机溶剂的混合物纯化6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的粗甲酯，得到纯的化合物（V）; e）用碱在有机溶剂中的溶液水解化合物（V），得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（Ⅵ）的金属盐。 f）使用有机或无机酸酸化阿达帕林（VI）的金属盐，得到粗制阿达帕林（I），和g）使用有机溶剂的混合物重结晶粗制阿达帕林（I），得到纯的阿达帕林（I）。

5. 发明申请

WO99010308A1 BIPHENYL DERIVATIVES SUBSTITUTED BY AN AROMATIC OR HETEROAROMATIC RADICAL AND PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：通过芳香或异位放射性药物和化妆品组合物取代的联苯衍生物
公开(公告)号：WO99010308A1
公开(公告)日：1999-03-04
申请号：PCT/FR1998/001834
申请日：1998-08-21
IPC分类号： C07D317/18 , A61K8/00 , A61K8/30 , A61K8/36 , A61K8/368 , A61K8/37 , A61K8/42 , A61K8/49 , A61K31/166 , A61K31/192 , A61K31/194 , A61K31/235 , A61K31/357 , A61K31/381 , A61K31/382 , A61K31/39 , A61K31/44 , A61K31/455 , A61K31/535 , A61P9/10 , A61P17/00 , A61P17/04 , A61P17/08 , A61P17/10 , A61P17/12 , A61P17/14 , A61P17/16 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61Q5/00 , A61Q19/00 , C07C13/48 , C07C63/49 , C07C65/17 , C07C65/26 , C07C69/76 , C07C69/94 , C07C233/64 , C07C233/65 , C07C235/42 , C07C259/10 , C07D213/79 , C07D213/80 , C07D265/22 , C07D317/22 , C07D327/06 , C07D333/38 , C07D335/06 , A61K31/19
CPC分类号： C07C65/26 , C07C65/17 , C07C69/94
摘要： The invention concerns compounds of formula (I) in which: Ar represents an aromatic radical or a heteroaromatic radical optionally substituted in particular by an alkyl or a carboxylic group; R2 and R3, represent in particular H, alkyl, or R2 and R3, together form a cycle with 5 or 6 chains; R4 and R5 represent in particular H or halogen; R6 represents in particular H or lower alkyl, and the salts of the compounds of formula (I). Said compounds can be used in particular for treating dermatological diseases related to keratinization disorder, and to fight against skin ageing.
摘要翻译：本发明涉及式（I）化合物，其中：Ar表示芳基或任选被烷基或羧基取代的杂芳基; R2和R3特别表示H，烷基或R2和R3一起形成具有5或6个链的循环; R4和R5特别表示H或卤素; R6代表特别是H或低级烷基，和式（I）化合物的盐。所述化合物特别可用于治疗与角质化障碍有关的皮肤病学疾病，并抵抗皮肤老化。

6. 发明申请

WO2015159098A1 FLUOROALKYLFLUORENE DERIVATIVES 审中-公开
标题翻译：氟代烷基衍生物
公开(公告)号：WO2015159098A1
公开(公告)日：2015-10-22
申请号：PCT/GB2015/051164
申请日：2015-04-17
申请人： LOMOX LIMITED
IPC分类号： C07D417/14 , C07C65/26 , C07C35/21 , C07C69/92 , C07C43/225 , C07D207/452 , C07D285/14 , H01L51/00
CPC分类号： H01L51/0039 , C07C43/225 , C07C65/21 , C07C69/593 , C07C69/60 , C07C69/92 , C07C2603/18 , C07D207/452 , C07D207/46 , C07D285/14 , C07D417/14 , C08G61/121 , C08G2261/146 , C08G2261/228 , C08G2261/312 , C08G2261/3142 , C08G2261/3221 , C08G2261/3223 , C08G2261/3246 , C08G2261/512 , C08G2261/53 , C08G2261/76 , C08G2261/91 , C08G2261/92 , C08G2261/95 , C09K11/025 , C09K19/32 , H01L51/0035 , H01L51/0036 , H01L51/005 , H01L51/0052 , H01L51/0068 , H01L51/0071 , H01L51/0076 , H01L51/0512 , H01L51/42 , H01L51/5012 , H01L51/5056 , Y02E10/549
摘要： There are provided compounds of the formula D-S 1- A-S 2 -B 1 wherein A comprises a 2,7- disubstituted 9,9-fluoroalkyl fluorene diradical of the formula wherein S 1 , S 2 , D and B 1 have meanings given in the description that are useful as charge transport and emissive materials for the fabrication of electronic devices such as diodes, transistors, and photovoltaic devices.
摘要翻译：提供式D-S1-A-S2-B1的化合物，其中A包含下式的2,7-二取代的9,9-氟烷基芴二价基团其中S1，S2，D和B1具有在描述中给出的含义，作为用于制造诸如二极管，晶体管和光伏器件的电子器件的电荷传输和发射材料是有用的。

7. 发明申请

WO2007125542A2 A PROCESS FOR PREPARATION OF ADAPALENE 审中-公开
标题翻译：一种制备ADAPALENE的方法
公开(公告)号：WO2007125542A2
公开(公告)日：2007-11-08
申请号：PCT/IN2007/000145
申请日：2007-04-09
申请人： USV LIMITED , TARUR, Radhakrishnan, Venkatasubramanian , BHISE, Nandu, Baban , SATHE, Dhananjay, Govind , PATNEKAR, Subodh, Shashikant , PATIL, Sachin, Shivaji
发明人： TARUR, Radhakrishnan, Venkatasubramanian , BHISE, Nandu, Baban , SATHE, Dhananjay, Govind , PATNEKAR, Subodh, Shashikant , PATIL, Sachin, Shivaji
IPC分类号： A61K31/192 , A61P17/10 , C07C41/16 , C07C43/225 , C07C51/09 , C07C67/343 , C07C65/26
CPC分类号： C07C67/343 , C07C41/16 , C07C51/09 , C07C51/412 , C07C2603/74 , C07C65/26 , C07C69/94 , C07C43/225
摘要： The present invention discloses a process for preparation of highly pure Adapalene, chemically designated as 6-[3-(l-adamantyl)-4-methoxy phenyl]-2-naphthoic acid (I) comprising: a) reacting 1-adamantanol with 4-bromophenol (II) in presence of sulphonic acid with or without the use of organic solvent to give 2-(l-adamantyl)-4- bromophenol (III); b) alkylating compound of formula(III) with dimethylsulphate in presence of base in organic solvent to obtain 2-(l-adamantyl)-4-bromoanisole (IV); c) C-C coupling the compound of formula (IV) with methyl-6-bromo-2- naphthoate using magnesium, purified zinc chloride and NiCl 2 -DPPE in THF at a temperature of 40-60°C tO obtain methyl ester of 6-[3-(l- adamantyl)-4-methoxy phenyl] -2-naphthoic acid (V); d) purifying crude methyl ester of 6-[3-(l-adamantyl)-4-methoxy phenyl]-2- naphthoic acid (V) using a mixture of organic solvent to obtain pure compound (V); e) hydrolyzing the compound (V) with a solution of alkali in organic solvent to obtain metal salt of 6-[3-(l-adamantyl)-4-methoxy phenyl] -2-naphthoic acid (VI); f) acidifying metal salt of adapalene (VI) using organic or inorganic acid to obtain crude adapalene (I) and g) recrystallizing the crude adapalene (I) using a mixture of organic solvents to obtain pure adapalene (I).
摘要翻译：本发明公开了一种高纯度阿达帕林的制备方法，化学命名为6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（I），包括： a）在磺酸存在下，使用或不使用有机溶剂，使1-金刚烷醇与4-溴苯酚（II）反应，得到2-（1-金刚烷基）-4-溴苯酚（III）; b）在碱存在下，在有机溶剂中，用硫酸二甲酯将式（III）化合物烷基化，得到2-（1-金刚烷基）-4-溴茴香醚（IV）; c）在THF中，在40-60℃的温度下，使用镁，纯化的氯化锌和NiCl 2 -DPEPE，使式（IV）的化合物与6-溴-2-萘甲酸甲酯偶联，得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的甲酯; d）使用有机溶剂的混合物纯化6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（V）的粗制甲酯以获得纯化合物（V）; e）用碱在有机溶剂中的溶液水解化合物（Ⅴ），得到6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸（Ⅵ）的金属盐。 f）使用有机酸或无机酸酸化阿达帕林（VI）的金属盐以获得粗制阿达帕林（I），和g）使用有机溶剂混合物使阿达帕林粗品（I）重结晶以获得纯阿达帕林（I）

8. 发明申请

WO2007072217A3 PROCESS FOR THE PREPARATION OF ADAPALENE AND RELATED COMPOUNDS 审中-公开
标题翻译：制备自由基和相关化合物的方法
公开(公告)号：WO2007072217A3
公开(公告)日：2007-11-01
申请号：PCT/IB2006003987
申请日：2006-06-16
申请人： MEDICHEM SA , PUIG SERRANO JORDI
发明人： PUIG SERRANO JORDI
IPC分类号： C07C43/21 , C07C65/26
CPC分类号： C07C65/26 , C07C51/02 , C07C51/09 , C07C51/412 , C07C51/43 , C07C51/47 , C07C51/50 , C07C67/343 , C07C2603/74 , C07C69/94
摘要： The invention provides an improved process for the preparation of a benzonaphthalene derivative including, in particular, the manufacture of high purity adapalene. The invention further includes a method for assessing the color of adapalene by means of a quantitative colorimetric measurement of the produced adapalene.
摘要翻译：本发明提供了一种制备苯并萘衍生物的改进方法，特别是制备高纯度阿达帕林。本发明还包括通过所产生的阿达帕林的定量比色测量来评估阿达帕林的颜色的方法。

9. 发明申请

WO0183438A3 NEW GAMMA SELECTIVE RETINOIDS 审中-公开
标题翻译：新游戏选择性反馈
公开(公告)号：WO0183438A3
公开(公告)日：2002-06-13
申请号：PCT/EP0104554
申请日：2001-04-23
申请人： HOFFMANN LA ROCHE
发明人： BELLONI PAULA NANETTE , JOLIDON SYNESE , KLAUS MICHAEL , LAPIERRE JEAN-MARC
IPC分类号： A61K31/045 , A61K31/11 , A61K31/165 , A61K31/19 , A61K31/192 , A61K31/20 , A61K31/23 , A61K31/235 , A61K31/27 , A61K31/275 , A61K31/353 , A61K31/381 , A61K31/382 , A61K31/421 , A61K31/4704 , A61P3/02 , A61P11/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/16 , A61P35/00 , A61P43/00 , C07C63/49 , C07C63/64 , C07C63/66 , C07C63/74 , C07C65/26 , C07C65/28 , C07C69/616 , C07C69/635 , C07C69/734 , C07C69/76 , C07C69/80 , C07C69/82 , C07C69/90 , C07C69/94 , C07C255/33 , C07C271/58 , C07C323/56 , C07C403/20 , C07D213/30 , C07D215/12 , C07D215/14 , C07D215/22 , C07D261/08 , C07D263/00 , C07D263/38 , C07D271/06 , C07D277/24 , C07D307/42 , C07D311/00 , C07D311/58 , C07D333/40 , C07D335/06
CPC分类号： C07D213/30 , C07C63/64 , C07C65/26 , C07C65/28 , C07C69/76 , C07C69/80 , C07C69/90 , C07C255/33 , C07C271/58 , C07C2602/10 , C07D215/14 , C07D261/08 , C07D271/06 , C07D277/24 , C07D307/42 , C07D311/58 , C07D333/40 , C07D335/06
摘要： New RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification, and pharmaceutically active salts of carboxylic acids of formula (I), further the invention relates to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor gamma (RAR gamma ) selective agonists for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.
摘要翻译：式（I）的新的RAR选择性类视黄醇激动剂，其中符号如说明书中所定义，和式（I）的羧酸的药学活性盐，本发明还涉及这种视黄酸受体激动剂，特别是视黄酸受体γ（RARγ）选择性激动剂，用于治疗肺气肿和相关的肺部疾病，以及治疗和预防皮肤病学障碍，用于治疗和预防恶性和恶化前上皮病变，肿瘤和粘膜前癌变化在口，舌，喉，食管，膀胱，子宫颈和结肠。

10. 发明申请

WO99058486A1 NEW COMPOUNDS, THEIR PREPARATION AND USE 审中-公开
标题翻译：新化合物，其制备和使用
公开(公告)号：WO99058486A1
公开(公告)日：1999-11-18
申请号：PCT/DK1999/000242
申请日：1999-05-04
IPC分类号： C07D335/06 , A61K31/192 , A61K31/352 , A61K31/382 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P3/10 , C07C51/09 , C07C57/50 , C07C59/72 , C07C63/49 , C07C63/66 , C07C65/26 , C07C67/343 , C07C69/76 , C07D213/54 , C07D213/80 , C07D215/12 , C07D311/58 , C07D401/10 , C07D405/10 , C07D409/10 , A61K31/19 , C07C63/44 , C07C65/24 , C07D213/24 , C07D213/60
CPC分类号： C07C59/72 , C07C57/50 , C07C63/66 , C07C65/26
摘要： The present invention provides novel compounds of general formula (I) wherein R , R , W, Z and R to R are defined more fully in the description. The compounds are useful in the treatment of ailments and disorders where a reduction of the blood glucose is beneficial, such as diabetes.
摘要翻译：本发明提供了通式（I）的新化合物，其中R 1，R 2，W，Z和R 5至R 9在本说明书中更充分地定义。该化合物可用于治疗血糖降低有益的疾病和疾病，例如糖尿病。

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