公开(公告)号：KR100377787B1

公开(公告)日：2003-03-26

申请号：KR1020000086254

申请日：2000-12-29

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김성훈 ,  남길수 ,  이정근 ,  이재목

IPC: C07D471/04

Abstract: PURPOSE: Provided are novel pyridopyrimidine derivatives which inhibit phosphodiesterase IV activity and TNF production. Also, provided are preparing process thereof and a pharmaceutical composition containing the same. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl amino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl; R is hydrogen, methyl, C3-7 lower alkyloxy, phenyl, benzyl, substituted phenyl(wherein a substituent group includes cyano, halogen, carboxylalkyl, nitro, methyl, trihalogenated ethyl or alkyloxy; and substitution site can be ortho-, meta-, or para- site), alkyloxy, C3-7 lower alkyloxy ethyl, benzyloxy, benzyloxyethyl, phenyloxyethyl, carboxyalkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生的新型吡啶并嘧啶衍生物。 另外，提供了其制备方法和含有其的药物组合物。 构成：新的吡啶并嘧啶衍生物由式（1）表示，其中R1为C1-3低级烷基，C3-7环烷基，环烷氧基，环烷基氨基，环烷基低级烷基，C1-3低级烷氧基，甲酰基，羟基低级烷基或 羧基; （其中取代基包括氰基，卤素，羧基烷基，硝基，甲基，三卤代乙基或烷氧基;取代位置可以是邻位，间位， 烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R4是氢或甲基，条件是R2和R3不相同。

公开(公告)号：KR1020050027453A

公开(公告)日：2005-03-21

申请号：KR1020030063730

申请日：2003-09-15

Applicant: 한국과학기술연구원

Inventor： 이상기 ,  이재균 ,  장용건 ,  이정근

IPC: C07F9/6503

CPC classification number: C07F19/00 ,  C07D233/14 ,  C07F9/5045 ,  C07F9/6506 ,  C07F15/008

Abstract: Chiral bisphosphine bearing imidazolium salt, their intermediates and a preparation method thereof are provided, which chiral bisphosphine forms chiral metal complex with transition metal ion, has high reactivity during asymmetric hydrogen reaction in ionic liquid, and improved photo-selectivity and conversion rate, and easily isolated and recovered after reaction. The chiral bisphosphine bearing imidazolium salt represented by formula (1) is provided, wherein n is an integer of 1 to 10; R1, R2, R3 and R4 are independently hydrogen, C1-C10 alkyl, C3-C8 cyclic alkyl, aryl or substituted aryl in which the substituent is halogen, C1-C6 alkyl or C1-C6 alkoxy; Z is phenyl or substituted aryl in which the substituent is halogen, C1-C6 alkyl or C1-C6 alkoxy; and X is BF4, PF6, SbF6, OTf or NTf2. The intermediates of the chiral bisphosphine bearing imidazolium salt represented by formula (1) are represented by formula (2), formula (3), formula (4), formula (5) and formula (6), respectively, wherein Y2 is halogen, methane sulfonyl or para-toluenesulfonyl.

Abstract translation: 提供手性双膦咪唑鎓盐及其制备方法，其中手性双膦与过渡金属离子形成手性金属络合物，在离子液体不对称氢反应中具有高反应性，并提高了光选择性和转化率 反应后分离并回收。 提供由式（1）表示的含有手性双膦的咪唑鎓盐，其中n为1至10的整数; R1，R2，R3和R4独立地是氢，C1-C10烷基，C3-C8环烷基，其中取代基是卤素的芳基或取代的芳基，C1-C6烷基或C1-C6烷氧基; Z是其中取代基是卤素，C 1 -C 6烷基或C 1 -C 6烷氧基的苯基或取代的芳基; X为BF4，PF6，SbF6，OTf或NTf2。 由式（1）表示的含有手性双膦的咪唑鎓盐的中间体分别由式（2），式（3），式（4），式（5）和式（6）表示，其中Y2是卤素， 甲磺酰或对甲苯磺酰。

公开(公告)号：KR1020020058217A

公开(公告)日：2002-07-12

申请号：KR1020000086254

申请日：2000-12-29

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김성훈 ,  남길수 ,  이정근 ,  이재목

IPC: C07D471/04

Abstract: PURPOSE: Provided are novel pyridopyrimidine derivatives which inhibit phosphodiesterase IV activity and TNF production. Also, provided are preparing process thereof and a pharmaceutical composition containing the same. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl amino, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl; R is hydrogen, methyl, C3-7 lower alkyloxy, phenyl, benzyl, substituted phenyl(wherein a substituent group includes cyano, halogen, carboxylalkyl, nitro, methyl, trihalogenated ethyl or alkyloxy; and substitution site can be ortho-, meta-, or para- site), alkyloxy, C3-7 lower alkyloxy ethyl, benzyloxy, benzyloxyethyl, phenyloxyethyl, carboxyalkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生的新型吡啶并嘧啶衍生物。 此外，提供其制备方法和含有其的药物组合物。 构成：新颖的吡啶并嘧啶衍生物由式（1）表示，其中R 1为C 1-3低级烷基，C 3-7环烷基，环烷氧基，环烷基氨基，环烷基低级烷基，C 1-3低级烷氧基，甲酰基，羟基低级烷基或 羧基; R为氢，甲基，C 3-7低级烷氧基，苯基，苄基，取代苯基（其中取代基包括氰基，卤素，羧基烷基，硝基，甲基，三卤代乙基或烷氧基;取代位点可以是邻位，间位， 或对位），烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R 4是氢或甲基，条件是R 2和R 3不相同。

公开(公告)号：KR100542868B1

公开(公告)日：2006-01-20

申请号：KR1020030063730

申请日：2003-09-15

Applicant: 한국과학기술연구원

Inventor： 이상기 ,  이재균 ,  장용건 ,  이정근

IPC: C07F9/6503

Abstract: 본 발명은 하기 화학식 1로 표시되는 이미다졸 염을 포함하는 키랄 비스포스핀에 전이금속이 배위된 전이금속착물, 이의 중간체 화합물 및 상기 전이금속착물의 제조방법에 관한 것이다.


(상기 화학식 1에서, n은 1~10의 정수이며, R
1 , R
2 , R
3 , R
4 는 서로 독립적이며, 수소, C
1 -C
10 알킬, C
3 -C
8 고리화 알킬, 아릴기 또는 치환된 아릴기를 나타내며, 이때 치환체는 할로겐, C
1 -C
6 알킬기 또는 C
1 -C
6 의 알콕시기이다.
Ar은 페닐 또는 치환된 아릴기를 나타내며, 이때 치환체는 할로겐, C
1 -C
6 알킬 또는 C
1 -C
6 의 알콕시기이다.
X는 BF
4 , PF
6 , SbF
6 , OTf, NTf
2 이다.)
본 발명의 키랄 비스포스핀은 전이금속이온과 키랄 금속착물을 형성하여, 청정용매인 이온성 액체 내에서 비대칭 촉매화 수소 환원 반응시 촉매로 작용하여 반응성이 크고, 광학선택성 및 전환율이 우수하며, 반응 후 촉매의 분리 및 회수가 용이하다.

公开(公告)号：KR100377788B1

公开(公告)日：2003-03-26

申请号：KR1020000086255

申请日：2000-12-29

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김성훈 ,  남길수 ,  이정근 ,  이재목

IPC: C07D471/04

Abstract: PURPOSE: Provided is a novel pyridopyrimidine derivative inhibiting phosphodiesterase IV activity, and TNF generation and its side effects. Also, provided are its manufacturing method and a pharmaceutical composition containing it. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is aryl, substituted aryl(wherein, a substitution group can be C1-3 lower alkyl group, C1-3 lower alkoxy group, halogen, aryl, or substituted aryl), aryl oxy, aryl amino, aryl substituted lower alkyl, pyridine, alkyl substituted pyridine, halogen substituted pyridine, C1-3 lower alkyl ester, substituted hetero cycle, hetero cycle oxy, hetero cycle, or amino hetero cycle lower alkyl; R2 hydrogen, C3-7 lower alkyl oxy, phenyl, benzyl, or substituted phenyl(wherein, a substitution group can be cyano, halogen, carboxy alkyl, methyl, trihalogenated methyl, or alkyl oxy, and substitution site can be ortho-, para-, or meta- site), alkyl oxy, C3-7 lower alkyl oxy ethyl, benzyl oxy, benzyl oxy ethyl, phenyl oxy ethyl, carboxy alkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

Abstract translation: 目的：提供抑制磷酸二酯酶IV活性和TNF产生及其副作用的新型吡啶并嘧啶衍生物。 另外，提供了其制造方法和含有它的药物组合物。 构成：新的吡啶并嘧啶衍生物由式（1）表示，其中R1为芳基，取代的芳基（其中，取代基可以为C1-3低级烷基，C1-3低级烷氧基，卤素，芳基或取代的 芳基氧基，芳基氨基，芳基取代的低级烷基，吡啶，烷基取代的吡啶，卤素取代的吡啶，C 1-3低级烷基酯，取代的杂环，杂环氧基，杂环或氨基杂环低级烷基; 苯基，苄基或取代的苯基（其中，取代基可以是氰基，卤素，羧基烷基，甲基，三卤代甲基或烷基氧基，取代位置可以是邻位，对位 - 或间位），烷氧基，C 3-7低级烷氧基乙基，苄氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R4是氢或甲基，条件是R2和R3不相同。

公开(公告)号：KR1020020058218A

公开(公告)日：2002-07-12

申请号：KR1020000086255

申请日：2000-12-29

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김성훈 ,  남길수 ,  이정근 ,  이재목

IPC: C07D471/04

Abstract: PURPOSE: Provided is a novel pyridopyrimidine derivative inhibiting phosphodiesterase IV activity, and TNF generation and its side effects. Also, provided are its manufacturing method and a pharmaceutical composition containing it. CONSTITUTION: The novel pyridopyrimidine derivative is represented by the formula(1), wherein R1 is aryl, substituted aryl(wherein, a substitution group can be C1-3 lower alkyl group, C1-3 lower alkoxy group, halogen, aryl, or substituted aryl), aryl oxy, aryl amino, aryl substituted lower alkyl, pyridine, alkyl substituted pyridine, halogen substituted pyridine, C1-3 lower alkyl ester, substituted hetero cycle, hetero cycle oxy, hetero cycle, or amino hetero cycle lower alkyl; R2 hydrogen, C3-7 lower alkyl oxy, phenyl, benzyl, or substituted phenyl(wherein, a substitution group can be cyano, halogen, carboxy alkyl, methyl, trihalogenated methyl, or alkyl oxy, and substitution site can be ortho-, para-, or meta- site), alkyl oxy, C3-7 lower alkyl oxy ethyl, benzyl oxy, benzyl oxy ethyl, phenyl oxy ethyl, carboxy alkyl or cyano group; and R4 is hydrogen or methyl group, provided that R2 and R3 are not the same.

Abstract translation: 目的：提供抑制磷酸二酯酶IV活性的新型吡啶并嘧啶衍生物，以及TNF的产生及其副作用。 此外，其制造方法和含有它的药物组合物。 构成：新颖的吡啶并嘧啶衍生物由式（1）表示，其中R1为芳基，取代芳基（其中取代基可为C1-3低级烷基，C1-3低级烷氧基，卤素，芳基或取代基 芳基氧基，芳基氨基，芳基取代的低级烷基，吡啶，烷基取代的吡啶，卤素取代的吡啶，C1-3低级烷基酯，取代的杂环，杂环氧，杂环或氨基杂环低级烷基; R 2氢，C 3-7低级烷基氧基，苯基，苄基或取代的苯基（其中，取代基可以是氰基，卤素，羧基烷基，甲基，三卤代甲基或烷氧基，取代位点可以是邻位，对位 - 或间位），烷基氧基，C 3-7低级烷基氧基乙基，苄基氧基，苄氧基乙基，苯氧基乙基，羧基烷基或氰基; 并且R 4是氢或甲基，条件是R 2和R 3不相同。