公开(公告)号：KR101052066B1

公开(公告)日：2011-07-27

申请号：KR1020080104760

申请日：2008-10-24

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  유경호 ,  오창현 ,  조승주 ,  정세진 ,  엘-딥이브리엄무스타파 ,  박병선

IPC: C07D403/04

Abstract: 본 발명은 신규의 6-(피리딘-3-일)피리미딘 화합물과 약제학적으로 허용 가능한 이의 염, 이 화합물의 제조방법, 그리고 이 화합물을 항암제로 사용하는 의약적 용도에 관한 것이다.
6-(피리딘-3-일)피리미딘 화합물, 항암제

Abstract translation: 本发明涉及新的6-（吡啶-3-基）嘧啶化合物，其药学上可接受的盐，制备该化合物的方法，以及该化合物作为抗癌药物的药物用途。

公开(公告)号：KR1020110007830A

公开(公告)日：2011-01-25

申请号：KR1020090065466

申请日：2009-07-17

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  유경호 ,  오창현 ,  한동근 ,  엘-딥이브리엄무스타파 ,  박병선 ,  정수진

IPC: C07D231/04 ,  C07D231/02

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

Abstract: PURPOSE: A novel pyrazole compound I provided to ensure excellent activity on ROS kinase enzyme and to suppress development of glioblastoma multiforma, CNS cancer, and brain cancer. CONSTITUTION: A pyrazole compound is denoted by chemical formula 1. A pharmaceutical composition for anti-cancer contains the pyrazole compound. An anticancer agent contains the pyrazole compound as an active ingredient. The anticancer agent is used for treating brain cancer, CNS caner, and glioblastoma multiforma. A method for preparing the pyrazole compound comprises: a step of reacting a hetero aromatic compound of chemical formula 3 with methyl 3-methoxy-5-methoxybenzoate compound of chemical formula 2 under the presence of lithium hexamethyldisilazide(LHMDS) to obtain a keto-enol tautomer compound; and a step of reacting the keto-enol tauotmer compound with hydrazine hydrate under anhydrous ethanol condition.

Abstract translation: 目的：提供一种新的吡唑化合物I，以确保对ROS激酶的优异活性，并抑制多形性胶质母细胞瘤，CNS癌和脑癌的发展。 构成：吡唑化合物由化学式1表示。用于抗癌的药物组合物含有吡唑化合物。 抗癌剂含有吡唑化合物作为活性成分。 抗癌剂用于治疗脑癌，CNS癌和多形性成胶质细胞瘤。 制备吡唑化合物的方法包括：使化学式3的杂芳族化合物与化学式2的3-甲氧基-5-甲氧基苯甲酸甲酯在六甲基二硅叠氮化锂（LHMDS）存在下反应，得到酮 - 烯醇 互变异构体 以及在无水乙醇条件下使酮 - 烯醇葡聚糖化合物与水合肼反应的步骤。

公开(公告)号：KR1020100064520A

公开(公告)日：2010-06-15

申请号：KR1020080122999

申请日：2008-12-05

Applicant: 한국과학기술연구원 ,  한국화학연구원 ,  한국생명공학연구원

Inventor： 심태보 ,  손정범 ,  김환 ,  박동식 ,  최환근 ,  함영진 ,  하정미 ,  유경호 ,  오창현 ,  이소하 ,  하재두 ,  조성윤 ,  권병목 ,  한동초

IPC: C07D231/56

CPC classification number: C07D413/14 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: PURPOSE: A pharmaceutical composition containing novel indazole derivatives is provided to suppress various protein kinases and to prevent and treat abnormal cell proliferative disorders. CONSTITUTION: A novel indazole derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating abnormal cell proliferative disorder contains indazole derivative of chemical formula 1, pharmaceutically acceptable salt, hydrate, or solvate. The indazole derivative of chemical formula 1 suppresses protein kinase of raf, KDR, Fms, Tie2, SAPK2a, or Ret. The abnormal cell proliferative disorder includes uterine cervix cancer, head and neck cancer, esophageal cancer, thyroid cancer, parathyroid cancer, kidney cancer, breeding, prostate cancer, urethral carcinoma, bladder cancer, and blood cancer.

Abstract translation: 目的：提供含有新型吲唑衍生物的药物组合物以抑制各种蛋白激酶，并预防和治疗异常细胞增殖性疾病。 构成：化学式1表示新的吲唑衍生物。用于预防和治疗异常细胞增殖病症的药物组合物含有化学式1的吲唑衍生物，药学上可接受的盐，水合物或溶剂合物。 化学式1的吲唑衍生物抑制raf，KDR，Fms，Tie2，SAPK2a或Ret的蛋白激酶。 异常细胞增殖障碍包括子宫颈癌，头颈癌，食管癌，甲状腺癌，甲状旁腺癌，肾癌，育种，前列腺癌，尿道癌，膀胱癌和血癌。

公开(公告)号：KR1020100045694A

公开(公告)日：2010-05-04

申请号：KR1020080104760

申请日：2008-10-24

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  유경호 ,  오창현 ,  조승주 ,  정세진 ,  엘-딥이브리엄무스타파 ,  박병선

IPC: C07D403/04

Abstract: PURPOSE: A novel 6-(pyridine-3-yl)primidine compound is provided to ensure anti-cancer activity and suppress melanoma development. CONSTITUTION: A novel 6-(pyridine-3-yl)pyrimidine compound is denoted by chemical formula 1. In chemical formula 1, R1 is hydrogen atom or C1-C6 alkyl group; R2 is hydrogen atom, halogen atom, phenyl amino group, phenyl group, acetylphenyl group, acetyl aminophenyl group, or pyridyl group; and Y is -N(R')C(O)-, -N(R')C(O)N(R")-, or -N(R')C(O)N(R")C(O)-. An anti-cancer drug contains the 6-(pyridine-3-yl)pyrimidine compound or pharmaceutically acceptable salt thereof.

Abstract translation: 目的：提供新的6-（吡啶-3-基）基基配合物以确保抗癌活性并抑制黑素瘤发展。 构成：化学式1表示新的6-（吡啶-3-基）嘧啶化合物。在化学式1中，R 1为氢原子或C 1 -C 6烷基; R2是氢原子，卤素原子，苯基氨基，苯基，乙酰基苯基，乙酰基氨基苯基或吡啶基; 并且Y是-N（R'）C（O） - ， - N（R'）C（O）N（R“） - 或-N（R'）C（O）N（R” O） - 。 抗癌药含有6-（吡啶-3-基）嘧啶化合物或其药学上可接受的盐。

公开(公告)号：KR1020100028992A

公开(公告)日：2010-03-15

申请号：KR1020080109444

申请日：2008-11-05

Applicant: 한국과학기술연구원

Inventor： 이소하 ,  류재천 ,  유경호 ,  엘-딥이브리엄무스타파

IPC: C07D239/32 ,  C07D239/34

Abstract: PURPOSE: A diphenylamine derivative having light emitting property is provided to ensure light emitting property by UV RAY or visible ray and use in organic electro luminescence device or electronic element for display. CONSTITUTION: A diphenylamine is denoted by chemical formula 1. In chemical formula 1, R1 and R2 are dependently hydrogen stom, C1-C8 alkyl group, substituted or non-substituted paenylgroup, biphenyl group. An organic electroluminescent (EL) device or display contains the pigment. A method for preparing palladium(Pd) diphenylamine derivative comprises: a first step of synthesizing ethanone compound of chemical formula 4 under the presence of catalyst and nitrogen; a second step of reacting ethanone compound of chemical formula 4 with N,N-dimethylformamide dimethylacetal to synthesize prophenone compound of chemical formula 5; a third step of reacting the prophenone compound with sodium ethoxide and guanidine hydrochloride to obtain amine compound of chemical formula 1a; and a step of reacting the amine compound with halide compound of R1-X or R2-X.

Abstract translation: 目的：提供具有发光性的二苯胺衍生物，以通过UV RAY或可见光确保发光特性，并用于有机电致发光元件或显示用电子元件。 构成：二苯胺由化学式1表示。在化学式1中，R 1和R 2是氢气，C 1 -C 8烷基，取代或未取代的苯基，联苯基。 有机电致发光（EL）装置或显示器含有颜料。 制备钯（Pd）二苯胺衍生物的方法包括：在催化剂和氮气存在下合成化学式4的乙酮化合物的第一步; 使化学式4的乙酮化合物与N，N-二甲基甲酰胺二甲缩醛反应合成化学式5的丙酮化合物的第二步; 使丙酮化合物与乙醇钠和盐酸胍反应的第三步骤，得到化学式1a的胺化合物; 以及使胺化合物与R1-X或R2-X的卤化物反应的步骤。

公开(公告)号：KR100847554B1

公开(公告)日：2008-07-21

申请号：KR1020060119502

申请日：2006-11-30

Applicant: 한국과학기술연구원

Inventor： 김경곤 ,  박남규 ,  이소하 ,  김동찬 ,  정세진

IPC: C07F15/00

Abstract: 본 발명은 시스-디(티오시아나토)-N,N'-비스(2,2'-비피리딜-4,4'-디카르복시산)루테늄(Ⅱ)의 개선된 제조방법에 관한 것으로서, 더욱 상세하게는 디메틸포름아미드(DMF) 또는 디메틸포름아미드(DMF) 수용액을 반응용매로 사용하고, 반응물질로서 루테늄(Ⅲ) 클로라이드 수화물, 2,2'-비피리딘-4,4'-디카르복시산 및 티오시안산 알칼리금속염을 한꺼번에 반응용기에 넣고 마이크로파를 조사하는 조건에서 환류 반응시켜 제조하며, 반응이 완결되면 반응용액에 염산 또는 황산의 무기산 수용액을 첨가하여 반응용액의 pH를 2 내지 5로 조절하는 간단한 분리공정을 수행하여 염료감응 태양전지용 N3 염료로 잘 알려져 있는 시스-디(티오시아나토)-N,N'-비스(2,2'-비피리딜-4,4'-디카르복시산)루테늄(Ⅱ)을 고체 상으로 수득하는 방법에 관한 것이다.
N3 염료, 염료감응 태양전지, 시스-디(티오시아나토)-N,N'-비스(2,2'-비피리딜-4,4'-디카르복시산)루테늄(Ⅱ), 루테늄(Ⅲ) 클로라이드 수화물, 2,2'-비피리딘-4,4'-디카르복시산, 티오시안산 알칼리금속염

公开(公告)号：KR100613407B1

公开(公告)日：2006-08-17

申请号：KR1020040073914

申请日：2004-09-15

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하 ,  표정인 ,  노관호

IPC: C07D491/048 ,  C07D495/04

Abstract: 본 발명은 유기 전계발광소자용 피리미딘 유도체에 관한 것으로서, 더욱 상세하게는 피리미딘을 모핵으로 하고 여기에 다양한 전자 주게 및 전자 끌게 치환체가 치환되어 있는 신규 구조의 물질로서 청색 발광현상을 나타내므로 유기 전계발광소자로 유용한 피리미딘 유도체에 관한 것이다.
유기 전계 발광소자, 피리미딘 유도체, 유기 OLED.

公开(公告)号：KR100400885B1

公开(公告)日：2003-10-17

申请号：KR1020010043741

申请日：2001-07-20

Applicant: 경동제약 주식회사 ,  한국과학기술연구원

Inventor： 이병석 ,  정찬성 ,  이소하 ,  김영희

IPC: C07D487/04

Abstract: PURPOSE: A separating method of a single isomer from the ketorolac of the racemic body is provided, thereby separating the high purity of a single isomer form ketorolac. CONSTITUTION: The separating method of a single isomer from the ketorolac of the racemic body comprises the steps of: reaction of the ketorolac of the racemic body represented by formula(1) with alcohol compounds in the presence of Candida antartica lipase B; and separation of (-)-isomer from the reaction mixture by absorption, wherein the alcohol compounds are C3 to C20 alcohols; the amount of the Candida antartica lipase B is 10 to 150 wt.%; and the reaction temperature is 20 to 70 deg. C.

Abstract translation: 目的：提供从外消旋体的酮咯酸中分离单一异构体的方法，由此分离单一异构体形式的酮咯酸的高纯度。 构成：从外消旋体的酮咯酸中分离单一异构体的方法包括以下步骤：使由式（1）表示的外消旋体的酮咯酸与醇化合物在南极假丝酵母脂肪酶B存在下反应; 和通过吸收从反应混合物中分离（ - ） - 异构体，其中醇化合物是C 3 -C 20醇; 南极假丝酵母脂肪酶B的量为10至150重量％; 反应温度为20〜70℃。 C。

公开(公告)号：KR100379755B1

公开(公告)日：2003-04-11

申请号：KR1020000064693

申请日：2000-11-01

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하

IPC: C07C25/00

Abstract: PURPOSE: A process for producing butanamides having optical activity is provided, thereby easily producing butanamides useful as an intermediate in manufacturing antimicrobial agents, herbicides or medicines, in higher yield. CONSTITUTION: The process for producing butanamides having optical activity comprises the steps of: resolving racemic 4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2) into (3R)-(+)-4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2a) and (3S)-(-)-4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2b) using R-(+)-methylbenzylamine of formula(3); and reacting each divided compound of formula(2a) or formula(2b) with aniline derivative of formula(5) to produce butanamide derivative of formula(1).

Abstract translation: 目的：提供一种生产具有光学活性的丁酰胺的方法，由此容易以较高的收率制备可用作制备抗微生物剂，除草剂或药物的中间体的丁酰胺。 构成：具有光学活性的丁酰胺的制备方法包括以下步骤：将式（2）的外消旋4-苯基-3-（4-苯氧基苯基）丁酸转化为（3R） - （+） - 4-苯基-3- （+） - 甲基苄胺制备式（2a）的（4-苯氧基苯基）丁酸和（3S） - （ - ） - 4-苯基-3-（4-苯氧基苯基）丁酸 3）; （2a）或式（2b）的每种分开的化合物与式（5）的苯胺衍生物反应以产生式（1）的丁酰胺衍生物。

公开(公告)号：KR1020020034017A

公开(公告)日：2002-05-08

申请号：KR1020000064693

申请日：2000-11-01

Applicant: 한국과학기술연구원

Inventor： 정찬성 ,  이소하

IPC: C07C25/00

Abstract: PURPOSE: A process for producing butanamides having optical activity is provided, thereby easily producing butanamides useful as an intermediate in manufacturing antimicrobial agents, herbicides or medicines, in higher yield. CONSTITUTION: The process for producing butanamides having optical activity comprises the steps of: resolving racemic 4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2) into (3R)-(+)-4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2a) and (3S)-(-)-4-phenyl-3-(4-phenoxyphenyl) butanoic acid of formula(2b) using R-(+)-methylbenzylamine of formula(3); and reacting each divided compound of formula(2a) or formula(2b) with aniline derivative of formula(5) to produce butanamide derivative of formula(1).

Abstract translation: 目的：提供具有光学活性的丁酰胺的制造方法，从而容易地制造用作制造抗微生物剂，除草剂或药物中的较高产率的中间体的丁酰胺。 制备具有光学活性的丁酰胺的方法包括以下步骤：将式（2）的外消旋4-苯基-3-（4-苯氧基苯基）丁酸分解成（3R） - （+） - 4-苯基-3- 式（2a）的（4-苯氧基苯基）丁酸和式（2b）的（3S） - （ - ） - 4-苯基-3-（4-苯氧基苯基）丁酸使用式 3）; 并使式（2a）或式（2b）的每一个分开的化合物与式（5）的苯胺衍生物反应得到式（1）的丁酰胺衍生物。