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81.发明授权
公开(公告)号：KR100490970B1
公开(公告)日：2005-05-24
申请号：KR1020020015728
申请日：2002-03-22
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：KR100377788B1
公开(公告)日：2003-03-26
申请号：KR1020000086255
申请日：2000-12-29
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。
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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
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。
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Patent Agency Ranking
公开(公告)号：KR1020020058218A
公开(公告)日：2002-07-12
申请号：KR1020000086255
申请日：2000-12-29
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。
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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
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。
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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
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。
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公开(公告)号：KR1020010073360A
公开(公告)日：2001-08-01
申请号：KR1020000001703
申请日：2000-01-14
Applicant: 한국과학기술연구원
IPC: C07D277/34
Abstract: PURPOSE: Provided is a method for producing 2-penacylidene- 3,5- alkyl substituted-1,3- thiazolidine-4-on easily under mild condition. CONSTITUTION: The 2-penacylidene- 3,5- alkyl substituted-1,3- thiazolidine-4-on represented by the formula (1) is produced by reacting thiopenacyl keten S,N-acetal represented by the formula (2) with alpha-haloacylhalogen represented by the formula (3), in which R1 is C1 to C6 alkyl, C7 to C8 arylalkyl, C7 to C8 arylalkyl having an aromatic ring substituted by substituents selected from the group consisting of C1 to C3 alkyl, C1 to C3 alkoxy and halogen, and C5 to C7 cycloalkyl; R2 is hydrogen or C1 to C3 lower alkyl; R3 is C1 to C6 alkyl, benzyl, benzyl having an aromatic rings substituted by substituents selected from the group consisting of C1 to C3 alkyl, C1 to C3 alkoxy, halogen and dialkylamino; and X is fluoride, chloride, bromide or iodide.
Abstract translation: 目的：提供在温和条件下容易地制备2-亚苄基-3,5-烷基取代-1,3-噻唑烷-4-酮的方法。 构型：由式（1）表示的2-缩水亚烷基-3,5-烷基取代的1,3-噻唑烷-4-酮通过将由式（2）表示的硫代萘酰基酮酮S，N-缩醛与α （3）表示的卤代酰卤，其中R 1为C 1至C 6烷基，C 7至C 8芳烷基，具有被选自C 1至C 3烷基，C 1至C 3烷氧基的取代基取代的芳环的C 7至C 8芳烷基 和卤素，和C5至C7环烷基; R2是氢或C1-C3低级烷基; R3是C1至C6烷基，苄基，具有被选自C1至C3烷基，C1至C3烷氧基，卤素和二烷基氨基的取代基取代的芳环的苄基; X是氟化物，氯化物，溴化物或碘化物。
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公开(公告)号：KR100139021B1
公开(公告)日：1998-04-30
申请号：KR1019950002382
申请日：1995-02-09
Applicant: 한국과학기술연구원
IPC: C07H15/236
CPC classification number: C07H15/12
Abstract: 본 발명은 양자성 용매하에 킬레이트화제를 사용하여 시소마이신을 킬레이트화하고, 킬레이트화된 시소마이신의 3,2',6' 위치의 아미노기를 아실화제로서 아실화반응에 의해 보호하고, 암모니아수로 킬레이트화된 금속을 이탈시킨 다음, 얻어진 3,2,'6'-트리치환 시소마이신을 비양자성 유기용매에서 에틸화제와 반응시켜 1 위치의 아미노기만을 선택적으로 에틸화시키고, 이어서 탈보호하는 것으로 이루어진 다음 구조식(I)의 1-N-에틸시소마이신 및 그의 약리학적 허용염의 제조방법을 제시한다:
상기 1-N-에틸시소마이신은 인체의 감염증을 치료하는데 사용되는 아미노글리코시드계의 항생제이며, 본 발명의 제조방법에 따라 고수율로 얻어진다.
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