公开(公告)号：KR100490970B1

公开(公告)日：2005-05-24

申请号：KR1020020015728

申请日：2002-03-22

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김중협 ,  최경일 ,  남길수 ,  서재홍 ,  이재목 ,  송석범 ,  이건호 ,  전형옥

IPC: C07D471/04

Abstract: 본 발명은 다음의 일반식 (I)로 표시되는 신규한 피리도[2,3-d]피리미딘 카르보알데히드 옥심계 화합물 또는 약학적으로 허용되는 이들의 염, 이들의 제조방법 및 이들의 선택적 포스포디에스테라아제 IV 효소 활성 억제 효과에 의한 약리학적 적용에 관한 것이다.

(I)

公开(公告)号：KR1020020095286A

公开(公告)日：2002-12-26

申请号：KR1020010033382

申请日：2001-06-14

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김유승 ,  최경일 ,  김동현 ,  남길수 ,  서재홍

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: PURPOSE: Provided is a method for preparing novel pyrazolpyrimidine derivative represented by the formula(1) and its pharmaceutically acceptable salts or hydrates. A pharmaceutical composition containing it is used as a therapeutic agent for impotency by inhibition of phosphodiesterase V. CONSTITUTION: The novel pyrazolpyrimidine derivative represented by the formula(1), wherein R1 and R2 are independently C1-C6 alkyl or C3-C6 cycloalkyl; R3 is substituted or unsubstituted C1-C6 alkyl, C3-C6 cycloalkyl or C3-C6 alkenyl; and X is O or NR4 wherein R4 is hydrogen, OH or C1-C6 alkyl, C3-C6 cycloalkyl or C3-C6 alkenyl substituted or unsubstituted by alkoxy group. It is manufactured by the steps of: converting pyrazolopyrimidinone of the formula(2) into pyrazolopyrimidinethione of the formula(3) by thione reaction; chlorosulfonating the compound of the formula(3) into chlorosulfone compound of the formula(4) and letting the compound of formula(4) react with secondary amine to make the final compound of the formula(1).

Abstract translation: 目的：提供由式（1）表示的新型吡唑嘧啶衍生物及其药学上可接受的盐或水合物的制备方法。 通过抑制磷酸二酯酶V将含有它的药物组合物用作阳性的治疗剂。构成：由式（1）表示的新型吡唑嘧啶衍生物，其中R 1和R 2独立地为C 1 -C 6烷基或C 3 -C 6环烷基; R3是取代或未取代的C1-C6烷基，C3-C6环烷基或C3-C6烯基; 且X为O或NR 4，其中R 4为氢，OH或C 1 -C 6烷基，C 3 -C 6环烷基或被烷氧基取代或未取代的C 3 -C 6烯基。 其通过以下步骤制备：通过硫酮反应将式（2）的吡唑并嘧啶酮转化为式（3）的吡唑并嘧啶硫酮; 将式（3）的化合物氯化为式（4）的氯砜化合物，并使式（4）的化合物与仲胺反应以制备式（1）的最终化合物。

公开(公告)号：KR1020010075920A

公开(公告)日：2001-08-11

申请号：KR1020000002868

申请日：2000-01-21

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김성훈 ,  남길수 ,  서재홍

IPC: C07D413/08

Abstract: PURPOSE: Provided is a novel oxazolidinone derivative which includes a thiophene ring and has antibacterial effects on gram positive bacterial. Also, its pharmaceutically acceptable salt and hydrate are provided. CONSTITUTION: A novel oxazolidinone derivative or its pharmaceutically acceptable salt and hydrates includes a thiophene ring and is represented by the formula (1). in the formula, R1 is a phenyl group or halogen, a phenyl group of which an alkoxy group is substituted; R2 is a saturated alkyl group of C1-4 or an alkyl group of C1-3 of which one hydrogen is substituted with a phenyl group, a cycloalkyl group of C3-8, a benzyl group of which an aryl group is substituted with an alkyl group of C1-3; and R3 is hydrogen or fluorine. The compound of the formula (1) is prepared by reacting a compound of the formula (2) with a compound of formula (3).

Abstract translation: 目的：提供一种新颖的恶唑烷酮衍生物，其包含噻吩环，对革兰氏阳性细菌具有抗菌作用。 此外，提供其药学上可接受的盐和水合物。 构成：一种新的恶唑烷酮衍生物或其药学上可接受的盐和水合物包括噻吩环并由式（1）表示。 在该式中，R 1是苯基或卤素，其中烷氧基被取代的苯基; R2是C1-4的饱和烷基或其一个氢被苯基取代的C1-3烷基，C3-8的环烷基，其中一个芳基被烷基取代的苄基 C1-3组; R3是氢或氟。 式（1）的化合物通过使式（2）的化合物与式（3）的化合物反应来制备。

公开(公告)号：KR1020010073620A

公开(公告)日：2001-08-01

申请号：KR1020000002382

申请日：2000-01-19

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김성훈 ,  남길수 ,  장관영 ,  서재홍

IPC: C07D501/16

CPC classification number: Y02P20/55

Abstract: PURPOSE: A pyrazolopyridine substituted cephalosporin compound is provided, which have the wide antimicrobial activity for gram positive and gram negative bacteria. And a producing method thereof is also provided. CONSTITUTION: The pyrazolopyridine substituted cephalosporin compound is represented by formula (1), in which R1 is hydrogen, C1 to C3 alkyl, C1 to C3 alkyl containing hydroxy, C1 to C3 alkyl containing amine; and R2 is hydrogen, amino, amino protected by amine protecting groups, carboxy or its inorganic salts, carbarmoyl, C1 to C3 alkyl substituted carbarmoyl, C1 to C3 alkyl containing hydroxy, and C1 to C3 alkyl esterified carboxy. The method for producing the pyrazolopyridine substituted cephalosporin compounds comprises the steps of: reacting the compounds of formula (2) and (3); and deprotecting R3 and R4, in which R3 is amine protecting groups, R4 is carboxylic acid protecting groups; and Y is halogen or acetoxy.

Abstract translation: 目的：提供吡唑并吡啶取代的头孢菌素化合物，对革兰氏阳性菌和革兰氏阴性菌具有广泛的抗菌活性。 并提供其制造方法。 构成：吡唑并吡啶取代的头孢菌素化合物由式（1）表示，其中R1为氢，C1至C3烷基，含羟基的C1至C3烷基，含C1至C3烷基的胺; 羧基或其无机盐，氨甲酰基，C 1至C 3烷基取代的氨甲酰基，含C 1至C 3烷基的羟基和C 1至C 3烷基酯化羧基保护的氨基。 制备吡唑并吡啶取代的头孢菌素化合物的方法包括以下步骤：使式（2）和（3）的化合物反应; 并使R3和R4脱保护，其中R3是胺保护基，R4是羧酸保护基; Y为卤素或乙酰氧基。

公开(公告)号：KR1020030076073A

公开(公告)日：2003-09-26

申请号：KR1020020015729

申请日：2002-03-22

Applicant: 한국과학기술연구원 ,  씨제이 주식회사

Inventor： 김중협 ,  최경일 ,  남길수 ,  서재홍 ,  이재목 ,  송석범 ,  이건호 ,  전형옥

IPC: C07D471/04

Abstract: PURPOSE: Pyrido£2,3-d|pyridine-2,4-dione aminomethyl derivatives useful as PDE IV inhibitor and a preparation method thereof are provided, which compounds are useful for treatment of respiration diseases, and diseases associated with TNF(tumor necrosis factor) formation. CONSTITUTION: Pyrido£2,3-d|pyridine-2,4-dione aminomethyl derivatives represented by formula (I) or pharmaceutically acceptable salts are provided, wherein R1 is C1-3 lower alkyl, C3-7 cycloalkyl, cycloalkyloxy, cycloalkyl lower alkyl, C1-3 lower alkoxy, formyl, hydroxy lower alkyl or carboxyalkyl, phenyl or X-substituted phenyl, in which X is methyl, ethyl, propyl, isopropyl, methoxy, ethoxy, propoxy, isopropoxy, cyano, carboxylic acid, carboxymethyl ester, carboxyethyl ester, nitro, fluoro or trifluoromethyl; R2 is C1-3 lower alkyl, C3-7 cycloalkyl, hydroxy, C1-6 lower alkylhydroxy, benzyl, X-substituted phenyl, C1-3 lower alkylphenyl, C1-3 lower alkyl substituted pyridine, C1-3 lower alkyl imidazol, morpholine, C1-3 lower alkyl morpholine, C1-3 lower alkyl piperazine, 4-substituted C1-3 lower alkyl piperazine in which the substituent is hydroxyethyl or methyl, alkylpyrrol or N-substituted alkylpyrrol, in which X is cyano, halogen, carboxyalkyl, nitro, methyl, trihalogenated methyl or alkyloxy; and R3 is hydrogen or methyl, and R2 and R3 are the same or different together. A method for preparing pyrido£2,3-d|pyridine-2,4-dione aminomethyl derivatives of formula (I) comprises preparing a compound of formula (III) from a compound of formula (II), and reducing the compound of formula (III).

Abstract translation: 目的：提供用作PDE IV抑制剂的吡啶2,3-d-吡啶-2,4-二酮氨基甲基衍生物及其制备方法，该化合物可用于治疗呼吸疾病和与TNF相关的疾病（肿瘤坏死 因子）形成。 构成：提供由式（I）表示的吡啶并[2,3-d]吡啶-2,4-二酮氨基甲基衍生物或其药学上可接受的盐，其中R 1为C 1-3低级烷基，C 3-7环烷基，环烷氧基，环烷基低级 烷基，C 1-3低级烷氧基，甲酰基，羟基低级烷基或羧基烷基，苯基或X取代的苯基，其中X是甲基，乙基，丙基，异丙基，甲氧基，乙氧基，丙氧基，异丙氧基，氰基，羧酸， ，羧乙基酯，硝基，氟或三氟甲基; R2是C1-3低级烷基，C3-7环烷基，羟基，C1-6低级烷基羟基，苄基，X取代的苯基，C1-3低级烷基苯基，C1-3低级烷基取代的吡啶，C1-3低级烷基咪唑，吗啉 ，C 1-3低级烷基吗啉，C 1-3低级烷基哌嗪，其中取代基为羟乙基或甲基的4-取代的C 1-3低级烷基哌嗪，其中X为氰基，卤素，羧基烷基， 硝基，甲基，三卤代甲基或烷氧基; 并且R 3是氢或甲基，并且R 2和R 3在一起是相同或不同的。 制备式（I）的吡啶并[2,3-d]吡啶-2,4-二酮氨基甲基衍生物的方法包括由式（II）化合物制备式（III）的化合物，还原式 （III）。

公开(公告)号：KR100380323B1

公开(公告)日：2003-04-16

申请号：KR1020000003695

申请日：2000-01-26

Applicant: 한국과학기술연구원

Inventor： 김중협 ,  김성훈 ,  남길수 ,  서재홍

IPC: C07D501/16

Abstract: PURPOSE: Provided is a novel cephalosporin which has an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at position number 3, and shows antibacterial activity against various gram positive bacteria and gram negative bacteria. CONSTITUTION: The cephalosporin is characterized by having an amino thiazole derivative at the position number 7 and N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)amino group at the position number 3 and represented by formula (1). In formula (1), R represents a saturated alkyl group of C1-3 and an unsaturated alkene group of C3-5; R1 is hydrogen, or a saturated alkyl group of C1-3; and R2 represents hydrogen, carboxyl group(or the inorganic cation thereof), carbamoyl group, carbamoyl group of which one or two hydrogen are substituted with an alkyl group of C1-3, or carboxyl group esterified with alkyl group of C1-3. Also, R1 and R2 represent a ring structure linked with 3 to 5 methylene groups.

Abstract translation: 用途：提供了一种新型头孢菌素，其在7号位具有氨基噻唑衍生物，在3号位具有N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，并且显示出抗菌 对各种革兰氏阳性菌和革兰氏阴性菌的活性。 构成：头孢菌素的特征在于在位置7具有氨基噻唑衍生物，在位置3具有N-甲基-N-（3-甲基-1,3-噻唑鎓-2-基）氨基，并由式 （1）。 在式（1）中，R表示C1-3的饱和烷基和C3-5的不饱和烯基; R1是氢或C1-3的饱和烷基; R2表示氢，羧基（或其无机阳离子），氨基甲酰基，其中一个或两个氢被C1-3的烷基取代的氨基甲酰基或被C1-3的烷基酯化的羧基。 此外，R1和R2表示与3至5个亚甲基连接的环结构。