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1. 发明授权

KR100565002B1 Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 有权
标题翻译： N-苯基-2-嘧啶胺衍生物及其制备方法
公开(公告)号：KR100565002B1
公开(公告)日：2006-03-30
申请号：KR1020040017594
申请日：2004-03-16
申请人： 일양약품주식회사
发明人： 김동연 , 김재근 , 조대진 , 이공열 , 김홍엽 , 우석훈 , 배우철 , 이선애 , 한병철 , 김용석
IPC分类号： C07D401/14
CPC分类号： C07D401/04 , C07D401/12
摘要： 본 발명은 온혈 동물에서의 각종 암에 탁월한 효과를 나타내는 하기 화학식 1의 N-페닐-2-피리미딘-아민 유도체 및 그의 염, 그의 제조방법, 및 이 화합물을 활성 성분으로 함유함을 특징으로 하는 폐암, 위암, 대장암, 췌장암, 간암, 전립선암, 유방암, 만성 또는 급성 백혈병, 혈액암, 뇌종양, 방광암, 직장암, 자궁경부암 등 질병 치료용 약제학적 조성물에 관한 것이다.

상기 식에서 R
1 , R
2 , R
3 , R
4 , R
5 , R
6 , R
7 , 및 R
8 은 명세서에 정의된 바와 같다.

2. 发明公开

KR1020050025397A 신규한 암로디핀 염 및 그의 제조방법 无效
标题翻译： NOBLE AMLODIPINE SALTS及其制备方法
公开(公告)号：KR1020050025397A
公开(公告)日：2005-03-14
申请号：KR1020030062443
申请日：2003-09-08
申请人： 일양약품주식회사
发明人： 김동연 , 김재근 , 조대진 , 이공열 , 김홍엽 , 우석훈 , 이선애
IPC分类号： C07D211/90
摘要： Amlodipine salts and a method for preparing the same compounds are provided, which amlodipine salt is a crystalline acid added salt having improved physicochemical properties such as high pharmaceutical stability, non-hygroscopicity and tablet adherence, and low toxicity, so that the amlodipine salt can be useful as a composition for treatment of cardiovascular diseases. The amlodipine salts represented by formula (1) are provided, wherein R is selected from malonic acid, itaconic acid, 2-thiopen carboxylic acid, glutaric acid, sebacic acid, sorbic acid, malic acid and phthalic acid. The method for preparing the amlodipine salts comprises the steps of: (1) dissolving amlodipine of formula (2) in an organic solvent and cooling the reaction solution; (2) dissolving 0.1 to 5.0 equivalent of acid in an organic solvent, and adding the amlodiping dissolved solution of step (1) into the solution where the acid is dissolved to prepare a mixture; and (3) stirring the mixture at -10 to 50 deg. C, filtering the mixture, cleansing and drying the filtered solid contents, wherein the acid is selected from malonic acid, itaconic acid, 2-thiopen carboxylic acid, glutaric acid, sebacic acid, sorbic acid, malic acid and phthalic acid; and the solvent is selected from water, methanol, ethanol, isopropanol, ethylacetate or methylene chloride.
摘要翻译：提供氨氯地平盐和制备相同化合物的方法，其氨氯地平盐是具有改善的物理化学性质如药物稳定性，非吸湿性和片剂粘附性以及低毒性的结晶酸加成盐，使得氨氯地平盐可以是可用作治疗心血管疾病的组合物。提供由式（1）表示的氨氯地平盐，其中R选自丙二酸，衣康酸，2-硫辛酸羧酸，戊二酸，癸二酸，山梨酸，苹果酸和邻苯二甲酸。制备氨氯地平盐的方法包括以下步骤：（1）将式（2）的氨氯地平溶于有机溶剂中并冷却反应溶液; （2）在有机溶剂中溶解0.1〜5.0当量的酸，并将步骤（1）的悬浮液溶解溶液加入到溶解酸的溶液中以制备混合物; 和（3）在-10至50℃搅拌该混合物。过滤混合物，清洗并干燥过滤后的固体成分，其中酸选自丙二酸，衣康酸，2-硫代羧酸，戊二酸，癸二酸，山梨酸，苹果酸和邻苯二甲酸; 溶剂选自水，甲醇，乙醇，异丙醇，乙酸乙酯或二氯甲烷。

3. 发明授权

KR101148399B1 항궤양제 및 점막보호제를 함유하는 경구용 위장질환치료용 약제 조성물 有权
标题翻译：用于治疗含有抗凝和粘膜保护剂的胃病的药物组合物
公开(公告)号：KR101148399B1
公开(公告)日：2012-05-23
申请号：KR1020050053752
申请日：2005-06-22
申请人： 일양약품주식회사
发明人： 김동연 , 이준연 , 윤환민 , 이선애 , 한병철 , 박미선 , 신호영
IPC分类号： A61K31/4439 , C07D401/12
摘要： An oral gastric disease therapeutic composition is provided to show specifically excellent treating effect for the gastric diseases by comprising an anti-ulcerant and a bismuth preparation as a mucosal protective agent. The oral pharmaceutical composition comprises ilprazole as an anti-ulcerant and 30-98 wt.% of a bismuth preparation as a mucosal protective agent which is selected from the group consisting of colloidal bismuth sub-citrate, bismuth aluminate, bismuth sub-carbonate, bismuth citrate, bismuth gallate, bismuth nitrate, bismuth tartarate, and a mixture thereof.

4. 发明公开

KR1020060134232A 항궤양제 및 점막보호제를 함유하는 경구용 위장질환치료용 약제 조성물 有权
标题翻译：用于治疗含有抗精神病药物和粘膜保护剂的胃肠疾病的药物组合物
公开(公告)号：KR1020060134232A
公开(公告)日：2006-12-28
申请号：KR1020050053752
申请日：2005-06-22
申请人： 일양약품주식회사
发明人： 김동연 , 이준연 , 윤환민 , 이선애 , 한병철 , 박미선 , 신호영
IPC分类号： A61K31/4439 , C07D401/12
CPC分类号： A61K31/4439 , A61K9/0053 , A61K33/245 , Y10S514/925
摘要： An oral gastric disease therapeutic composition is provided to show specifically excellent treating effect for the gastric diseases by comprising an anti-ulcerant and a bismuth preparation as a mucosal protective agent. The oral pharmaceutical composition comprises ilprazole as an anti-ulcerant and 30-98 wt.% of a bismuth preparation as a mucosal protective agent which is selected from the group consisting of colloidal bismuth sub-citrate, bismuth aluminate, bismuth sub-carbonate, bismuth citrate, bismuth gallate, bismuth nitrate, bismuth tartarate, and a mixture thereof.
摘要翻译：提供口服胃病治疗组合物，通过包含抗溃疡剂和作为粘膜保护剂的铋制剂，显示出对胃疾病的特别优异的治疗效果。口服药物组合物包含作为抗溃疡剂的伊曲唑和30-98重量％的铋制剂作为粘膜保护剂，其选自胶体铋柠檬酸铋，铝酸铋，亚碳酸铋，铋柠檬酸盐，没食子酸铋，硝酸铋，酒石酸铋及其混合物。

5. 发明公开

KR1020050080965A 포스포디에스테라제 저해제로서 신규한피라졸로피리미디논 유도체 및 이의 제조방법 无效
标题翻译：新型吡唑并嘧啶酮衍生物作为磷酸二酯酶抑制剂及其制备方法
公开(公告)号：KR1020050080965A
公开(公告)日：2005-08-18
申请号：KR1020040009161
申请日：2004-02-12
申请人： 일양약품주식회사
发明人： 김동연 , 김재근 , 이준연 , 조귀형 , 박성태 , 김정우 , 편두혁 , 남상돈 , 이선애 , 한병철 , 박미선
IPC分类号： C07D487/04
摘要： 본 발명은 하기 화학식1로 표시되는 새로운 피라졸로피리미디논 유도체와 이의 제조방법에 관한 것으로,
더욱 상세하게는, 본 발명은 하기 화학식1의 신규한 피라졸로피리미디논 유도체를 이용하여 특히 cGMP-대사 포스포디에스테라제의 저해제로서 그의 약제학적 용도를 제공함으로써 기존의 약물보다 체내흡수가 빠르고 생체내 독성이 낮은 약물을 제공하는 특징이 있다.
[화학식1]

상기 화학식 1에서 R
1 , R
2 , R
3 , R
4 및 R
5 는 각각 발명의 상세한 설명에서 정의하는 바와 같다.

6. 发明公开

KR1020040095155A Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 有权
标题翻译：具有抗癌活性的N-苯基-2-吡啶胺衍生物，其用于治疗癌症及其制备方法
公开(公告)号：KR1020040095155A
公开(公告)日：2004-11-12
申请号：KR1020040017594
申请日：2004-03-16
申请人： 일양약품주식회사
发明人： 김동연 , 김재근 , 조대진 , 이공열 , 김홍엽 , 우석훈 , 배우철 , 이선애 , 한병철 , 김용석
IPC分类号： C07D401/14
CPC分类号： C07D401/04 , C07D401/12
摘要： PURPOSE: N-phenyl-2-pyrimidine-amine derivatives and a process for the preparation thereof are provided, which compounds have improved anti-cancer activity, so that it can be useful for treatment of cancers such as lung cancer, stomach cancer, colon cancer, pancreas cancer, liver cancer, prostate cancer, breast cancer, leukemia, blood cancer, brain cancer, bladder cancer, rectal cancer and cervix cancer. CONSTITUTION: The N-phenyl-2-pyrimidine-amine derivatives represented by formula (1) and pharmaceutically acceptable salts thereof are provided, wherein R1 is 3-pyridyl or 4-pyridyl; R2 and R3 are independently hydrogen or lower alkyl; R6 or R7 are substituted with a radical of formula (2); X is oxygen or NH; n is 0 or 1; and R9 is C5 to C10 aliphatic group, optionally substituted monocyclic radical which contains 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur, and 5- to 7-membered cyclic ring, optionally benzene ring fused bi- or tri-cyclic radical, or lower alkyl substituted piperazinyl or homopiperazinyl, wherein R4, R5, R7 and R8 are simultaneously hydrogen or one or two of them are independently halogen, lower alkyl or lower alkoxy when the radical of formula (2) is substituted with R6, and one or two of R4, R5, R6 and R8 are independently halogen, lower alkyl or lower alkoxy when the radical of formula (2) is substituted with R7, provided that one or more of R4, R5, R7 and R8, or one or more of R4, R5, R6 and R8 is halogen when R6 or R7 are substituted with the radical of formula (2) of which R9 is 4-methylpiperazine and n is 0.
摘要翻译：目的：提供N-苯基-2-嘧啶胺衍生物及其制备方法，该化合物具有改善的抗癌活性，因此其可用于治疗癌症，例如肺癌，胃癌，结肠癌症，胰腺癌，肝癌，前列腺癌，乳腺癌，白血病，血癌，脑癌，膀胱癌，直肠癌和子宫颈癌。构成：提供由式（1）表示的N-苯基-2-嘧啶 - 胺衍生物及其药学上可接受的盐，其中R1是3-吡啶基或4-吡啶基; R2和R3独立地是氢或低级烷基; R6或R7被式（2）的基团取代; X是氧或NH; n为0或1; 并且R 9为C 5至C 10脂族基团，任选取代的单环基团，其含有1-3个选自氮，氧和硫的杂原子，以及5-至7-元环，任选苯环稠合的双 - 或三 - 环基，或低级烷基取代的哌嗪基或高哌嗪基，其中当式（2）的基团被R6取代时，其中R4，R5，R7和R8同时为氢或一个或两个独立地为卤素，低级烷基或低级烷氧基，当式（2）的基团被R 7取代时，R 4，R 5，R 6和R 8中的两个独立地为卤素，低级烷基或低级烷氧基，条件是R 4，R 5，R 7和R 8中的一个或多个，当R6或R7被其中R9是4-甲基哌嗪并且n是0的式（2）的基团取代时，R4，R5，R6和R8是卤素。

7. 发明公开

KR1020070070292A 혈액순환 개선에 효과가 있는 동물생약 및 식물생약 조성물 无效
标题翻译：用于血液循环的动物和植物草本组合物
公开(公告)号：KR1020070070292A
公开(公告)日：2007-07-04
申请号：KR1020050032980
申请日：2005-04-21
申请人： 일양약품주식회사
发明人： 김동연 , 정원태 , 박선 , 이선애 , 박미선 , 김현미
IPC分类号： A61K35/646 , A61K35/62 , A61K35/64 , A61K36/258 , A61K36/65 , A61K9/20 , A61K9/48
CPC分类号： A61K35/646 , A61K9/20 , A61K9/48 , A61K35/62 , A61K35/63 , A61K36/258 , A61K36/65
摘要： An animal and plant herbal composition for improving blood circulation is provided to promote blood flow, relief blood coagulation and improve blood vessel hardening such as arteriosclerosis without side effects. The animal and plant herbal composition for improving blood circulation comprises animal herb medicines containing 10-18 wt.% of Buthus martensi(scorpion), 15-25 wt.% of Whitmania pigra Whitman, 10-15 wt.% of Cryptotympana pustulata, 5-12 wt.% of Scolopendra subspinipes mutilans and 13-19 wt.% of Eupolyphaga sinensis Walker, and plant herb medicines containing 10-15 wt.% of Panax ginseng, 12-17 wt.% of Paeoniae Radix and 1.8-4 wt.% of Dryobalanops aromatica Gaertner, wherein the composition is formulated as tablet or capsule.
摘要翻译：提供用于改善血液循环的动植物草药组合物，以促进血液流动，缓解血液凝固，改善血管硬化，如动脉硬化，无副作用。用于改善血液循环的动物和植物草药组合物包含含有10-18重量％的马蹄i（蝎子），15-25重量％的惠特马尼亚白猪（Whitmania pigra Whitman），10-15wt。％糠of（Cryptotympana pustulata），5 -12重量％的Scolopendra subspinipes mutilans和13-19重量％的Eupolyphaga sinensis Walker，以及含有10-15重量％人参，12-17重量％芍药和1.8-4重量％ DryBalanops aromatica Gaertner的％，其中组合物配制成片剂或胶囊。

8. 发明授权

KR100674813B1 Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 有权
标题翻译： N-苯基-2-吡啶胺衍生物及其制备方法
公开(公告)号：KR100674813B1
公开(公告)日：2007-01-29
申请号：KR1020050071656
申请日：2005-08-05
申请人： 일양약품주식회사
发明人： 김동연 , 조대진 , 이공열 , 김홍엽 , 우석훈 , 김용석 , 이선애 , 한병철
IPC分类号： C07D403/04 , C07D401/04 , C07D417/04
CPC分类号： C07D417/14 , C07D401/14 , C07D403/14
摘要： An N-phenyl-2-pyrimidine-amine derivative is provided to be effective for treating various cancers such as lung cancer, stomach cancer, large intestine cancer, pancreas cancer, liver cancer, prostatic carcinoma, breast cancer, chronic or acute leukemia, myelogenous leukemia, encephaloma, bladder cancer, rectal cancer, cervical cancer, and lymphoma. The N-phenyl-2-pyrimidine-amine derivative is represented by the formula(1), wherein R1 is substituted or unsubstituted thiazole, imidazole or pyrazine(where a substituent is amino or C1-6 alkyl), each R2, R3 and R6 is independently H, halogen, C1-6 alkyl or C1-6 alkoxy, each R4 and R5 is independently H, halogen C1-6 alkyl, C1-6 alkoxy, or a radical represented by the formula(2)(where R7 is C1-6 alkyl or C1-6 alkyl substituted by 1 to 3 halogen(s) and R8 is C5-10 aliphatic group, saturated or unsaturated monocyclic radical containing 1 to 3 hetero atom(s) selected from N, O and S and 5-7 numbered cyclic member, optionally benzene-ring fused non- or tri-cyclic radical, or piperazinyl or homo-piperazinyl substituted by C1-6 alkyl) provided that all of the R2, R3, R5 and R6 are H or one or two of them is independently halogen, C1-6 alkyl or C1-6 alkoxy when the R4 is the radical of the formula(2), and one or two of the R2, R3, R5 and R6 is independently halogen, C1-6 alkyl or C1-6 alkoxy when the R5 is radical of the formula(2). To prepare the compound of the formula(1), a compound represented by the formula(4a) or (4b) is reacted with a compound represented by the formula(5) to produce a compound represented by the formula(1a) or (1b).
摘要翻译：提供N-苯基-2-嘧啶胺衍生物可用于治疗各种癌症如肺癌，胃癌，大肠癌，胰腺癌，肝癌，前列腺癌，乳腺癌，慢性或急性白血病，骨髓瘤白血病，脑病，膀胱癌，直肠癌，子宫颈癌和淋巴瘤。 N-苯基-2-嘧啶胺衍生物由式（1）表示，其中R 1是取代或未取代的噻唑，咪唑或吡嗪（其中取代基是氨基或C 1-6烷基），每个R 2，R 3和R 6 独立地为H，卤素，C 1-6烷基或C 1-6烷氧基，每个R 4和R 5独立地为H，卤素C 1-6烷基，C 1-6烷氧基或由式（2）表示的基团（其中R 7为C 1 -6烷基或被1至3个卤素取代的C 1-6烷基，R 8是C 5-10芳族基团，含有1至3个选自N，O和S的杂原子的饱和或不饱和单环基团， 7号环状成员，任选苯环稠合的非或三环基团，或被C 1-6烷基取代的哌嗪基或高哌嗪基），条件是所有的R 2，R 3，R 5和R 6均为H或一个或两个当R4是式（2）的基团时，它们独立地是卤素，C 1-6烷基或C 1-6烷氧基，R 2，R 3，R 5和R 6中的一个或两个独立地是卤素，C 1-6烷基或C 1 -6烷氧基当R5是式（2）的基团时。为了制备式（1）的化合物，将由式（4a）或（4b）表示的化合物与式（5）表示的化合物反应以制备由式（1a）或（1b）表示的化合物）。

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