公开(公告)号：KR1020090084455A

公开(公告)日：2009-08-05

申请号：KR1020080010662

申请日：2008-02-01

Applicant: 일동홀딩스(주)

Inventor： 이석준 ,  김정민 ,  이석택 ,  강재훈

IPC: C07D417/04

Abstract: A method for manufacturing a quetiapine fumarate is provided to synthesize with high yield and high purity through 2-step of economic process without by-product. A method for manufacturing a quetiapine fumarate of structural formula 1 comprises: a step of reacting dibenzo[b,f][1,4]thiazepine-11(10H)-one with 1.0 equivalent of phosphorus trichloride under the presence of N,N-dimethylanyline; and a step reacting 11-chlorobenzo [b,f][1,4]thiazepine with 1-[2-(2-hydroxyethoxy)ethyl]piperazine to obtain 11-[4[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine(quietiapine).

Abstract translation: 提供富马酸喹硫平的制备方法，通过两步经济方法无副产物合成，产率高，纯度高。 制备结构式1的富马酸喹硫平的方法包括：使二苯并[b，f] [1,4]硫杂-11（10H） - 酮与1.0当量的三氯化磷在N， dimethylanyline; 和11-氯苯并[b，f] [1,4]硫杂与1- [2-（2-羟基乙氧基）乙基]哌嗪反应，得到11- [4 [2-（2-羟基乙氧基）乙基] -1 哌嗪基]二苯并[b，f]的[1,4]硫氮杂（quietiapine）。

公开(公告)号：KR1020090077091A

公开(公告)日：2009-07-15

申请号：KR1020080002835

申请日：2008-01-10

Applicant: 일동홀딩스(주)

Inventor： 강재훈 ,  박천호 ,  홍창성 ,  유승우

IPC: C07D215/233 ,  C07D239/88 ,  C07D263/32 ,  C07D277/66

Abstract: A compound activating a peroxisom proliferator-activated receptor (PPAR)-alpha and gamma is provided to use as a therapeutic agent which has blood pressure reducing effect and bioavailability with less side effect. A peroxisom proliferator-activated receptor (PPAR) agonist for preventing and treating diabetes comprises a compound of the chemical formula I, its racemic mixture, optical isomer or partial isomer or it pharmacologically allowable salt. In the chemical formula I, R1 is hydrogen, linear or branch C1-6 alkyl, R2 and R3 is hydrogen, linear or branch C1-6 alkyl, C1-6 alkoxy, A1, A2, and A3 is separately carbon, nitrogen, oxygen or sulfur atom, R4 is hydrogen, linear or branch C1-6 alkyl, linear or branch C2-6 alkenyl.

Abstract translation: 提供激活过氧化物酶体增殖物激活受体（PPAR）-α和γ的化合物作为具有降血压作用和生物利用度较低副作用的治疗剂。 用于预防和治疗糖尿病的过氧化物酶体增殖物激活受体（PPAR）激动剂包括化学式I的化合物，其外消旋混合物，旋光异构体或部分异构体或其药学上允许的盐。 在化学式I中，R 1是氢，直链或支链C1-6烷基，R2和R3是氢，直链或支链C1-6烷基，C1-6烷氧基，A1，A2和A3分别是碳，氮，氧 或硫原子，R 4是氢，直链或支链C 1-6烷基，直链或支链C 2-6烯基。

公开(公告)号：KR100848232B1

公开(公告)日：2008-07-24

申请号：KR1020070035907

申请日：2007-04-12

Applicant: 일동홀딩스(주)

Inventor： 강재훈 ,  박천호 ,  권진선 ,  홍창성

IPC: C07D413/10 ,  C07D413/14

CPC classification number: C07D413/10 ,  C07D413/14

Abstract: Novel heterocycle or alkoxyaminomethyl oxazolidinone derivatives are provided to improve antibacterial activity and range against gram positive and negative bacteria, Pseudomonas, etc., and inhibit growth of antibiotic-resistant bacteria, so that the compounds are useful for treatment of various bacteria infection symptoms. The novel heterocycle or alkoxyaminomethyl oxazolidinone derivatives represented by the formula(I) shows strong and wide range of antibacterial activity, wherein A is carbon or nitrogen; R1 is -CH2NHOR4; R2 is acetamide, formamide or triazole; R3 is methyl, trifluoromethyl, fluoromethyl, hydroxymethyl, hydroxymethyl, ethylcarboxymethyl, ethylcarboxylate, methylcarboxylate, acetyl, diethoxymethyl, t-butyldimethylsilyl, trimethylsilyl, carboxylic acid, carbamide, aldehyde, hydroxyoxime or nitrile; R4 is hydrogen, methyl, ethyl, t-butyl or benzyl; B is CR5 or nitrogen; and R5 is hydrogen or ethylcarboxylate. The compounds represented by the formula(7) are prepared by reacting compounds represented by the formula(6) with hydroxylamine hydrochloride, adding N- chlorosuccinylimide into the resulting product in the presence of base such as pyridine, and reacting alkyne compounds represented by the formula(11) with the resulting product.

Abstract translation: 提供了新的杂环或烷氧基氨基甲基恶唑烷酮衍生物，以提高抗革兰氏阳性和阴性细菌，假单胞菌等的抗菌活性和范围，并抑制抗生素抗性细菌的生长，使得该化合物可用于治疗各种细菌感染症状。 由式（I）表示的新颖的杂环或烷氧基氨基甲基恶唑烷酮衍生物显示出强的和广泛的抗菌活性，其中A是碳或氮; R1是-CH2NHOR4; R2是乙酰胺，甲酰胺或三唑; R3是甲基，三氟甲基，氟甲基，羟甲基，羟甲基，乙基羧甲基，乙基羧酸酯，甲基羧酸酯，乙酰基，二乙氧基甲基，叔丁基二甲基甲硅烷基，三甲基甲硅烷基，羧酸，脲基，羟基肟或腈。 R4是氢，甲基，乙基，叔丁基或苄基; B为CR5或氮; R5是氢或乙基羧酸盐。 由式（6）表示的化合物与盐酸羟胺反应制备式（7）表示的化合物，在碱如吡啶存在下，将N-氯代琥珀酰亚胺加入到所得产物中，并将式 （11）与所得产品。

公开(公告)号：KR100684081B1

公开(公告)日：2007-02-16

申请号：KR1020000056513

申请日：2000-09-26

Applicant: 일동홀딩스(주)

Inventor： 김기원 ,  강재훈 ,  이석준 ,  윤능민 ,  정명주 ,  이상용 ,  안진희

IPC: C07D265/36

Abstract: 본 발명에서는 다음 구조식 (Ⅲ)의 화합물을 3급 아민과 금속촉매 존재 하에 수소화반응시켜 다음 구조식(Ⅱ)의 화합물을 얻고, 구조식(Ⅱ)의 화합물을 유기금속촉매와 포름산, 트리에틸아민 공비혼합물의 존재 하에 유기 용매 중에서 반응시키는 것으로 이루어진 다음 구조식(Ⅰ)의 광학 활성 3,4-디하이드로벤즈옥사진 유도체의 제조방법을 제공한다.

본 발명에 따라 제조된 광학 활성 3,4-디하이드로벤즈옥사진 유도체는 그람음성균뿐만이 아니라 그람양성균에 대해서도 강한 항균활성을 나타내는 항균제의 제조에 유용한 중간체 화합물이다.
벤즈옥사진, 광학활성, 항균제, 중간체

公开(公告)号：KR1020060116552A

公开(公告)日：2006-11-15

申请号：KR1020050039006

申请日：2005-05-10

Applicant: 연세대학교 산학협력단 ,  일동홀딩스(주)

Inventor： 이승택 ,  강재훈 ,  김동한 ,  류성언 ,  박정대 ,  유승우 ,  조봉환 ,  지애리 ,  최승수

IPC: C07C237/10

Abstract: Provided is a N-formylhydroxylamine derivative, which selectively inhibits gelatinase-like metalloproteinases including MMP-2 and MMP-9, and has the effects of inhibiting infiltration of human HT-1080 fibrosarcoma cell line and tube formation of human umbilical vein endothelial cells. The N-formylhydroxylamine derivative is a compound represented by the following formula I or a pharmaceutically acceptable salt thereof. In the formula I, R1 is H, a linear or branched C1-C6 alkyl, halogen atom or hydroxyl; R2 is a linear or branched C1-C6 alkyl or benzyl; R3 is a linear or branched C1-C6 alkyl or benzyl; and R4 is H or a C1-C6 alkyl.

Abstract translation: 提供了N-甲酰基羟胺衍生物，其选择性地抑制包括MMP-2和MMP-9的明胶酶样金属蛋白酶，并且具有抑制人HT-1080纤维肉瘤细胞系的浸润和人脐静脉内皮细胞的管形成的作用。 N-甲酰基羟胺衍生物是由下式I表示的化合物或其药学上可接受的盐。 在式I中，R 1为H，直链或支链C 1 -C 6烷基，卤原子或羟基; R2是直链或支链C 1 -C 6烷基或苄基; R3是直链或支链C 1 -C 6烷基或苄基; R4为H或C1-C6烷基。

公开(公告)号：KR1020060111744A

公开(公告)日：2006-10-30

申请号：KR1020050034057

申请日：2005-04-25

Applicant: 일동홀딩스(주)

Inventor： 강재훈 ,  유승우 ,  이희열 ,  조봉환 ,  안경미

IPC: C07D211/58

CPC classification number: C07D211/58 ,  Y02P20/55

Abstract: A novel hydroxamic acid derivative as a peptide deformylase inhibitor and a manufacturing method thereof are provided to inhibit proliferation of pathogenic bacteria by inhibiting their protein biosynthesis and polypeptide maturation catalyzed by the peptide deformylase. The hydroxamic acid derivative represented by the formula(I) or its pharmaceutically acceptable salt is provided, wherein A is -C(=O)NHOH or -N(CHO)OH; R1 is hydrogen, C1-3 alkyl, C4-6 cycloalkyl, halogen or hydroxy; R2 is hydrogen, linear or branched C1-6 alkyl, linear or branched C1-6 alkene, C4-6 cycloalkyl, C4-6 heterocycle containing N or O, or benzyl; R3 is hydrogen, methyl, linear or branched C1-6 alkyl, linear or branched C1-6 alkene, C4-6 cycloalkyl, phenyl or benzyl; R4 is hydrogen, linear or branched C1-4 alkyl, C1-4 alkene, or hydroxy substituted C1-4 alkyl; Y is represented by the formula(IIa), formula(IIb) or formula(IIc); n is 0 or 1; and R5, R6, R7, R8 and R9 are each independently hydrogen, linear or branched C1-3 alkyl, hydroxy, alkoxy, acyl, acyloxy, halogen, cyano, nitro, amino, N,N-dimethylamino, phenyl, morpholine or formyl. The hydroxamic acid derivative represented by the formula(I) or its pharmaceutically acceptable salt is prepared by reacting compounds of the formula(III) with hydroxylamine or N- or O-protected hydroxylamine, and removing the protecting group.

Abstract translation: 提供了一种新颖的异羟肟酸衍生物作为肽变性酶抑制剂及其制备方法，通过抑制其由肽变性酶催化的蛋白质生物合成和多肽成熟来抑制致病菌的增殖。 提供由式（I）表示的异羟肟酸衍生物或其药学上可接受的盐，其中A是-C（= O）NHOH或-N（CHO）OH; R1是氢，C1-3烷基，C4-6环烷基，卤素或羟基; R2是氢，直链或支链C1-6烷基，直链或支链C1-6烯烃，C4-6环烷基，含有N或O的C4-6杂环或苄基; R 3是氢，甲基，直链或支链C 1-6烷基，直链或支链C 1-6烯烃，C 4-6环烷基，苯基或苄基; R4是氢，直链或支链C 1-4烷基，C 1-4烯烃或羟基取代的C 1-4烷基; Y由式（IIa），式（IIb）或式（IIc）表示; n为0或1; R 5，R 6，R 7，R 8和R 9各自独立地为氢，直链或支链C 1-3烷基，羟基，烷氧基，酰基，酰氧基，卤素，氰基，硝基，氨基，N，N-二甲基氨基，苯基，吗啉或甲酰基 。 由式（I）表示的异羟肟酸衍生物或其药学上可接受的盐通过使式（III）的化合物与羟胺或N-或O-保护的羟胺反应并除去保护基来制备。

公开(公告)号：KR1020060007535A

公开(公告)日：2006-01-26

申请号：KR1020040056354

申请日：2004-07-20

Applicant: 일동홀딩스(주)

Inventor： 강재훈 ,  서명원 ,  권재욱 ,  윤진영

IPC: C07C209/72 ,  C07C211/27

Abstract: 본 발명은 일반 구조식(3)으로 표시되는 3-할로-N-메틸-3-페닐프로필아민을 벤젠 및 루이스 산 촉매 존재 하에 반응시켜서 다음 화학식 [I]로 표시되는 N-메틸-3,3-디페닐프로필아민의 개량된 제조방법에 관한 것이다. 본 발명은 수소화 반응처럼 가압반응설비를 필요로 하거나 위험한 공정이 없이 전체적인 공정이 비교적 용이하며, 고수율 및 고순도로 목적화합물을 얻을 수 있기 때문에 경제적이며 공업적인 대량생산을 위해 적용이 가능하다. 일반 화학식 [I]의 화합물은 제 3세대 디하이드로피리딘 계열의 칼슘채널차단제(L-형태의 칼슘채널 길항물질)인 레르카니디핀의 합성의 핵심 중간체이다.

상기식에서 X는 염소 또는 브롬의 할로겐 원자이다.
3-할로-N-메틸-3-페닐 프로필아민, 레르카니디핀, N-메틸-3,3-디페닐프로필아민

公开(公告)号：KR100174117B1

公开(公告)日：1999-02-01

申请号：KR1019950061498

申请日：1995-12-28

Applicant: 일동홀딩스(주)

Inventor： 김기원 ,  강재훈 ,  유동식 ,  장무수 ,  유승우

IPC: C07D501/24

CPC classification number: C07D501/00 ,  Y02P20/55

Abstract: 본 발명은 그람 양성균 및 그람 음성균에 대하여 매우 우수한 항균작용을 지닌 일반식 (Ⅰ)의 새로운 세팔로스포린 유도체 및 그 제조방법, 및 이를 유효성분으로 함유하는 항균제 조성물을 제공한다.

상기에서, R
1a 는 수소, 또는 아미노 보호기이고 R
1b 수소, C
1-4 알킬기, C
2-4 알케닐기, C
2-4 알키닐기, 플루오로로 치환된 C
1-3 알킬기, 또는 치환되거나 치환되지 않은 카르복시알킬기 등으로서 특히 메틸기, 에틸기, 알릴기, 프로파질기, 플루오로메틸기, 2-플루오로에틸기, -C(CH
3 )
2 COOH기, -CH
2 COOH기가 바람직하며 Q는 탄소, 또는 질소이다.
R
2 , R
3 은 서로 같거나 다르며 각각은 C
1-3 알킬기, C
2-4 알케닐기, C
2-4 알키닐기, 히드록시기로 치환된 C
1-3 알킬기이고, R
4 는 다음과 같은 것들이며,

(R
5 는 수소, C
1-3 알킬기, 히드록시기로 치환된 C
1-3 알킬기, R
6 은 수소, C
1-3 알킬기, C
2-4 알케닐기, 아미노기, R
7 은 C
1-3 알킬기, 히드록시기로 치환된 C
1-3 알킬기, Y는 산소, 또는 황, 또는 질소이고, Z는 수소, C
1-3 알킬기, 염소, 또는 플루오로이다), X는 할로겐원자이다.
본 발명에 따른 상기 구조식(Ⅰ)의 화합물은 항균활성이 탁월하며, 그 독성이 낮아 새로운 항균제로서 크게 기대된다.

公开(公告)号：KR1020150127436A

公开(公告)日：2015-11-17

申请号：KR1020140054237

申请日：2014-05-07

Applicant: 일동홀딩스(주)

Inventor： 이승훈 ,  강대중 ,  강재훈

IPC: A61K35/74 ,  A61P17/00 ,  A23L33/00

CPC classification number: C12N1/20 ,  A23L2/52 ,  A23L33/00 ,  A23L33/10 ,  A23V2002/00 ,  A23Y2220/73 ,  A61K35/74

Abstract: 본발명은고분자다당바인더에컨쥬게이트된열사락토바실러스람노서스, 이의제조방법및 이의용도에관한것이다. 본발명의고분자다당바인더에컨쥬게이트된열사락토바실러스람노서스는아토피질환의치료효과가뛰어나며, 특히기존의유산균제가가지고있는장점막부착경쟁력을월등히개선하여, 스테로이드계약물과동등한수준으로아토피성피부염의예방, 개선또는치료효과를나타내기때문에산업상이용가능성이크다.

Abstract translation: 本发明涉及与多糖聚合物粘合剂缀合的热灭活的鼠李糖乳杆菌，其制备方法及其用途。 与本发明的多糖聚合物粘合剂结合的热灭活的鼠李糖乳杆菌对特应性疾病具有优异的治疗效果，特别是具有高的工业可利用性，因为现有乳酸菌具有的膜粘附竞争力显着提高，从而显示出 预防，减轻或治疗特应性皮炎与类固醇类药物水平相同的效果。

公开(公告)号：KR1020140115149A

公开(公告)日：2014-09-30

申请号：KR1020130029876

申请日：2013-03-20

Applicant: 일동홀딩스(주)

Inventor： 강대중 ,  김태윤 ,  강재훈

IPC: C12P19/04 ,  C08B37/08 ,  A61K31/728

CPC classification number: C08B37/0072 ,  A61K31/728 ,  A61L27/20 ,  A61L27/58 ,  A61L31/042 ,  A61L31/148 ,  C08L5/08 ,  C12P19/26 ,  C12R1/46 ,  C12P19/04

Abstract: The present invention relates to a method for manufacturing hyaluronic acid having low dissolving speed in the body and a composition for adhesion prevention comprising hyaluronic acid manufactured thereby. More specifically provided are a method for manufacturing hyaluronic acid having low dissolving speed in the body including a step for cultivating streptococcus dysgalactiae ID9103 strains (KCTC11818BP) in a culture ground where carbon source and nitrogen source are included and a composition for adhesion prevention comprising hyaluronic acid manufactured thereby. Hyaluronic acid manufactured by the manufacturing method of the present invention has an excellent effect in adhesion prevention due to having low dissolving speed in the body as 4 million Da to 10 million Da of highly polymerized hyaluronic acid. A composition of the present invention for adhesion prevention comprising hyaluronic acid manufactured by the manufacturing method of the present method can ameliorate problems of the existing composition for adhesion prevention including cross-linker and compound and problems of the existing hyaluronic acid.

Abstract translation: 本发明涉及一种在体内具有低溶解速度的透明质酸的制造方法以及由此制造的透明质酸组合物。 更具体地提供了一种在体内制造具有低溶解速度的透明质酸的方法，包括在含有碳源和氮源的培养基中培养不育乳杆菌ID9103菌株（KCTC11818BP）的步骤和包含透明质酸的粘合预防组合物 由此制造。 通过本发明的制造方法制造的透明质酸由于在体内具有低溶解速度而具有优异的粘合防止效果，作为400万Da至1000万Da的高度聚合的透明质酸。 通过本发明的制造方法制造的包含透明质酸的本发明的组合物可以改善包括交联剂和化合物在内的现有的粘合防止组合物的问题和现有的透明质酸的问题。