公开(公告)号：KR100565002B1

公开(公告)日：2006-03-30

申请号：KR1020040017594

申请日：2004-03-16

Applicant: 일양약품주식회사

Inventor： 김동연 ,  김재근 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈 ,  배우철 ,  이선애 ,  한병철 ,  김용석

IPC: C07D401/14

CPC classification number: C07D401/04 ,  C07D401/12

Abstract: 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.

公开(公告)号：KR1020040095155A

公开(公告)日：2004-11-12

申请号：KR1020040017594

申请日：2004-03-16

Applicant: 일양약품주식회사

Inventor： 김동연 ,  김재근 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈 ,  배우철 ,  이선애 ,  한병철 ,  김용석

IPC: C07D401/14

CPC classification number: C07D401/04 ,  C07D401/12

Abstract: 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.

Abstract translation: 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。

公开(公告)号：KR1020070074878A

公开(公告)日：2007-07-18

申请号：KR1020060002943

申请日：2006-01-11

Applicant: 일양약품주식회사

Inventor： 김동연 ,  김용석 ,  허연구 ,  배우철 ,  김현미

IPC: A61K36/07 ,  A61P35/00

Abstract: A composition of the mycelium extract of Phellinus linteus having stability in water absorption and being rapidly dissolved, and a preparing method thereof are provided to inhibit hardness of Phellinus linteus mycelium extract during storage by water absorption, delay of disintegration time and lowering of drug bioavailability. The composition for improving stability in water absorption and rapidly dissolving the mycelium extract of Phellinus linteus comprises 40-99.5 wt.% of the mycelium extract of Phellinus linteus and 0.5-60 wt.% of pregelatinized starch as an excipient, and is formulated as capsule. The Phellinus linteus mycelium extract composition is prepared by mixing the Phellinus linteus mycelium extract with pregelatinized starch to obtain tablets, pulverizing the tablet with dry granulation method to prepare granules, and directly filing the capsules with the granules without drying them.

Abstract translation: 提供了具有吸水稳定性并快速溶解的桑黄菌丝体提取物的组合物及其制备方法，其用于通过吸水，分解时间的延迟和药物生物利用度的降低来抑制沙门氏菌菌丝体提取物的硬度。 用于提高吸水稳定性并快速溶解桑黄菌丝体提取物的组合物包含40-99.5重量％的桑黄菌丝体提取物和0.5-60重量％预胶化淀粉作为赋形剂，并配制成胶囊 。 通过将沙门氏菌菌丝体提取物与预胶化淀粉混合得到片剂，用干法造粒法粉碎片剂，制备颗粒剂，并直接用颗粒填充胶囊，而不使其干燥，从而制备桑黄菌丝体提取物组合物。