公开(公告)号：KR101810988B1

公开(公告)日：2017-12-20

申请号：KR1020117015617

申请日：2009-12-18

Applicant: 페노미넘 디스커버리스 인코포레이티드

Inventor： 칸엠.아민 ,  우드파울엘. ,  구데노웨다이안 ,  만키디리시케쉬 ,  아이아오누퍼슨

IPC: C07C229/22 ,  C07C279/14 ,  C07C323/59 ,  C07D339/04 ,  C07F9/10 ,  A61K31/202 ,  A61K31/445

CPC classification number: C07C323/59 ,  C07C229/22 ,  C07C279/14 ,  C07D339/04 ,  C07F9/106

Abstract: 화학식(I)의 1-알킬, 2-아실글리세롤유도체의합성경로및 치료용도가기술된다. 이는포유동물생물학적시스템에투여되었을때, 시스템의에테르지질합성능력과무관하게특이적 sn-2 치환된에탄올아민플라스말로겐의 세포내농도를증가시킨다. 이방법으로특이적 sn-2 치환된종의수준을상승시키는것은막 콜레스테롤수준을낮추고아밀로이드분비를저하시킬수 있다. 이들화합물은퇴행성신경질환(알쯔하이머병, 파킨슨병, 및연령-관련된황반변성을포함), 인식장애, 치매, 암(예, 전립선암, 폐암, 유방암, 난소암, 및신장암포함), 골다공증, 조울증및 혈관질병(예를들어, 동맥경화증, 고콜레스테롤혈증포함)과같은증가된막 콜레스테롤, 증가된아밀로이드, 및증가된플라스말로겐수준과관련된노화질병을치료하거나예방하는데사용될수 있다.

公开(公告)号：KR1020100101660A

公开(公告)日：2010-09-17

申请号：KR1020107015636

申请日：2008-12-12

Applicant: 에자끼구리고가부시키가이샤 ,  가부시키가이샤 나노에그

Inventor： 스기모토카즈히사 ,  니시우라히로미 ,  야마구치요코 ,  히라타케이이치 ,  쿠보타요시키

IPC: B82B3/00 ,  H01F1/055 ,  H01F1/053

CPC classification number: C07D339/04 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/14 ,  A61K9/2018 ,  A61K9/5115 ,  B82Y5/00

Abstract: 본 발명은 안정한 α-리포산에 관한 것이다. 또한 본 발명은 α-리포산과 비 이온성 계면활성제를 포함하는 수성 분산액을 제조하는 단계; 수성 분산액 속에 2가 금속염을 첨가하는 단계, 여기서 2가 금속염은 2가 금속 할로겐화물, 2가 금속 아세트산염 또는 2가 금속 글루콘산염이며; 그리고 2가 금속염이 첨가된 수성 분산액 속에 알칼리 금속 탄산염 또는 알칼리 금속 인산염을 첨가하여 α-리포산 나노입자들을 형성하는 단계를 포함하여 α-리포산 나노입자들을 제조하는 방법에 관한 것이다.

公开(公告)号：KR100935554B1

公开(公告)日：2010-01-07

申请号：KR1020090056337

申请日：2009-06-24

Applicant: 주식회사 셀트리온제약 ,  주식회사 셀트리온화학연구소

Inventor： 김경수 ,  박영준 ,  송현남 ,  이인숙 ,  김준우

IPC: C07D339/02 ,  C07D339/00

CPC classification number: C07D339/02 ,  C07D295/027 ,  C07D339/04

Abstract: PURPOSE: A pharmaceutical composition containing piperazine dithioctate is provided to ensure high solubility and stability to heat and moisture and prevent or treat multiple neuritis. CONSTITUTION: A piperazine dithioctate which is a novel basic additive salt of thioctic acid is denoted by chemical formula I. The thioctic acid is racemic form. The thioctic acid is R-(+)-thioctic acid or S-(-)-thioctic acid. The diffraction angle value of crystalline piperazine dithioctate is 13.9±0.2, 16.3±0.2, 17.1±0.2, 17.3±0.2, 18.2±0.2, 18.9±0.2, 20.5±0.2, 22.2±0.2, 22.8±0.2, 24.2±0.2, and 39.3±0.2. A pharmaceutical composition contains the piperazine dithioctate and pharmaceutically acceptable carrier. The pharmaceutical composition is used for treating or preventing multiple neuritis, dementia, Alzheimer, rheumatoid arthritis or suppressing increase of lipid in blood vessel.

Abstract translation: 目的：提供含有哌嗪二硫辛酸酯的药物组合物，以确保对热和水分的高溶解度和稳定性，并预防或治疗多种神经炎。 构成：硫辛酸的新型碱性添加盐的哌嗪二硫代酸盐由化学式I表示。硫辛酸为外消旋形式。 硫辛酸是R - （+） - 硫辛酸或S - （ - ） - 硫辛酸。 结晶哌嗪二硫辛酸酯的衍射角值为13.9±0.2,16.3±0.2,17.1±0.2,17.3±0.2,18.2±0.2,18.9±0.2,20.5±0.2,22.2±0.2,22.8±0.2,24.2±0.2 39.3±0.2。 药物组合物含有哌嗪二硫代辛酸酯和药学上可接受的载体。 药物组合物用于治疗或预防多种神经炎，痴呆，阿尔茨海默氏症，类风湿性关节炎或抑制血管中脂质的增加。

公开(公告)号：KR100822533B1

公开(公告)日：2008-04-16

申请号：KR1020037004735

申请日：2001-10-08

Applicant: 라보라토리오 치미코 인터나지오날레 에스.피.에이.

Inventor： 살비안니바레 ,  마이오라나스테파노 ,  코르첼라프란체스코

IPC: C07D339/04

CPC classification number: C07D339/04

Abstract: Process for the synthesis of racemic thioctic acid comprising the following stages: a) reaction of the alkyl ester of 6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis selected from the group consisting of quaternary ammonium or phosphonium salts having the following general formula: where: A is nitrogen of phosphorus, X is selected from the group consisting of Cl, Br, I, HSO4, and H2PO4 and the substitutents R1, R2, R3 and R4 are selection from the group consisting of linear or branched alkyl radicals having one to twenty carbon atoms (C1-C20), said substituents being identical or different one from the other, or only one of said substituents is selected from the group consisting of arylalkyl radicals having the following formula -(CH2)nC6H5 in which n=1-16; b) followed by the hydrolysis of the ester of racemic thiotic acid.

公开(公告)号：KR101267020B1

公开(公告)日：2013-05-30

申请号：KR1020077023878

申请日：2006-03-21

Applicant: 라보라토리오 치미코 인터나지오날레 에스.피.에이.

Inventor： 살비안니발레 ,  나르디안토니오 ,  브루노지아코모

IPC: C07D339/04

CPC classification number: C07D339/04

Abstract: 하기단계를포함하는티옥트산(thioctic acid) 정제방법: a) 알칼리성수 용액에상기티옥트산을용해하거나또는택일적으로는그의염을용해하고알칼리성 pH로적당하게맞추는단계, b) 상기단계 (a)로부터얻은용액을황산, 인산, 메탄술폰산으로이루어진군으로부터선택되는산으로 pH 5.4 내지 5.8로산성화하는단계, c) 상기단계 (b)에서침전된티옥트산을통상적인방법으로분리하는단계.

公开(公告)号：KR100838922B1

公开(公告)日：2008-06-16

申请号：KR1020037004733

申请日：2001-10-08

Applicant: 라보라토리오 치미코 인터나지오날레 에스.피.에이.

Inventor： 빌라니플라비오 ,  나르디안토니오 ,  살비안니바레 ,  파라벨라지오반나

IPC: C07D339/04

CPC classification number: C07D339/04 ,  C07C319/06 ,  C07C323/60

Abstract: Process for the synthesis of R(+)alpha-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(+)alpha-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)alpha-lipoic acid-R(+)alpha-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+) alpha-lipoic acid-R(+)alpha-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(+)alpha-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.

公开(公告)号：KR1020080031216A

公开(公告)日：2008-04-08

申请号：KR1020077030493

申请日：2006-03-31

Applicant: 안티브 홀딩스 인크.

Inventor： 월러스,존,엘. ,  치리노,쥬세페 ,  카리엔도,쥬세페 ,  스파라톨,안나 ,  산타가다,빈센초 ,  피오루치,스테파노

IPC: C07C333/02 ,  C07C327/40 ,  C07F9/6578

CPC classification number: C07C327/42 ,  C07C323/12 ,  C07C323/59 ,  C07C323/60 ,  C07C327/48 ,  C07D339/04 ,  C07F9/6578 ,  C07F9/6587

Abstract: The present invention provides new derivatives of 4-or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4-or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4-or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer.

Abstract translation: 本发明提供4-或5-氨基水杨酸的新衍生物，以及含有这些4-或5-氨基水杨酸衍生物作为活性成分的药物组合物，其可用于治疗肠疾病如炎性肠病（IBD）和 肠易激综合征（IBS）和预防/治疗结肠癌。 更具体地说，这些衍生物包括通过偶氮，酯，酸酐，硫酯或酰胺键与4-或5-氨基水杨酸的分子连接的硫化氢释放部分。 此外，本发明提供了制备这些化合物的方法及其用于治疗IBD和IBS以及预防/治疗结肠癌的用途。

公开(公告)号：KR1020060132903A

公开(公告)日：2006-12-22

申请号：KR1020067015988

申请日：2005-01-07

Applicant: 장피트

Inventor： 꼬몽-베르트랑,꺄린느 ,  들로멜,쟝-프랑수와

IPC: C07C323/12 ,  C07C323/22 ,  C07C323/61 ,  C07D339/04

CPC classification number: C07C323/12 ,  C07C59/90 ,  C07C323/22 ,  C07C2601/14 ,  C07D339/04

Abstract: The invention relates to substituted 1,3-diphenylprop-2-en-1-one derivative compounds, pharmaceutical and/or cosmetic compositions containing same, and the applications thereof in therapeutics and cosmetics. The invention also relates to a method of preparing said derivatives.

Abstract translation: 本发明涉及取代的1,3-二苯基丙-2-烯-1-酮衍生物化合物，含有它们的药物和/或化妆品组合物及其在治疗和化妆品中的应用。 本发明还涉及制备所述衍生物的方法。

公开(公告)号：KR1020060011936A

公开(公告)日：2006-02-06

申请号：KR1020057008064

申请日：2003-10-31

Applicant: 라보라토리오 치미코 인터나지오날레 에스.피.에이.

Inventor： 살비안니바레 ,  빌라니플라비오 ,  나르디안토니오 ,  데안제리스브루노

IPC: C07D339/04 ,  C07C229/22

CPC classification number: C07D339/04 ,  A23L33/10 ,  A23V2002/00 ,  A23V2250/026 ,  A23V2250/0612

Abstract: Salt of thioctic acid with L-carnitine with the formula: A Y (X)x where A is formula (I) where Y is the cation of an alkaline metal, of an alkaline earth metal or is a quaternary ammonium group, X is A or OH-, x is equal to 0 when Y is the cation of an alkaline metal or a quaternary ammonium group and equal to 1 when Y is an alkaline earth metal.

Abstract translation: 硫辛酸与L-肉碱的盐，具有下式：AY（X）x其中A是式（I）其中Y是碱金属阳离子，碱土金属或季铵基，X是A或 OH-时，当Y为碱金属或季铵基的阳离子时x等于0，当Y为碱土金属时，x等于1。

公开(公告)号：KR1020050057270A

公开(公告)日：2005-06-16

申请号：KR1020057003969

申请日：2003-09-08

Applicant: 고쿠리츠켄큐카이하츠호진 카가쿠기쥬츠신코키코 ,  고쿠리츠 다이가쿠 호우진 카고시마 다이가쿠

Inventor： 슈다,야수오 ,  아라노,아키오 ,  큐슈모토,소이치 ,  소벨,마이클

IPC: C07D339/02 ,  C07D339/04

CPC classification number: C07H15/04 ,  A61K47/549 ,  C07D339/04 ,  C07D409/14 ,  Y10S435/961 ,  Y10S435/97

Abstract: A linker compound having a structure represented by the following general formula (1): (1) wherein n is an integer of 1 to 6, and wherein X has a structure being a multi-branched structure moiety comprising three or four hydrocarbon chains which has an aromatic amino group at the terminal thereof and may contain a carbon- nitrogen bond in the main chain thereof; and a ligand which comprises the linker compound and a saccharide introduced therein.

Abstract translation: 具有由以下通式（1）表示的结构的连接体化合物：（1）其中n是1至6的整数，并且其中X具有包含三个或四个烃链的多支链结构部分的结构，其具有 在其末端具有芳香族氨基，并且在其主链中可以含有碳 - 氮键; 以及包含连接体化合物和引入其中的糖的配体。